Tag: M.W=450-500

Yang, Chengbin published the artcileDiscovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity, SDS of cas: 757978-19-1, the publication is ACS Medicinal Chemistry Letters (2017), 8(8), 875-880, database is CAplus and MEDLINE.

The phosphoinositide 3-kinase (PI3K) inhibitors potently inhibit the signaling pathway of PI3K/AKT/mTOR, which provides a promising new approach for the molecularly targeted cancer therapy. In this work, a novel series of 7-azaindole scaffold derivatives was discovered by the fragment-based growing strategy. The structure-activity relationship profiles identified that the 7-azaindole scaffold derivatives exhibit potent activity against PI3K at mol. and cellular levels as well as cell proliferation in a panel of human tumor cells.

ACS Medicinal Chemistry Letters published new progress about 757978-19-1. 757978-19-1 belongs to iodides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Bromide,Iodide,Sulfamide,Benzene, name is 5-Bromo-3-iodo-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine, and the molecular formula is C10H9ClN2O, SDS of cas: 757978-19-1.

Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Miles, Dillon H. published the artcileDiscovery of Potent and Selective 7-Azaindole Isoindolinone-Based PI3Kγ Inhibitors, Category: iodides-buliding-blocks, the publication is ACS Medicinal Chemistry Letters (2020), 11(11), 2244-2252, database is CAplus and MEDLINE.

The successful application of immunotherapy in the treatment of cancer relies on effective engagement of immune cells in the tumor microenvironment. Phosphoinositide 3-kinase γ (PI3Kγ) is highly expressed in tumor-associated macrophages, and its expression levels are associated with tumor immunosuppression and growth. Selective inhibition of PI3Kγ offers a promising strategy in immuno-oncol., which has led to the development of numerous potent PI3Kγ inhibitors with variable selectivity profiles. To facilitate further investigation of the therapeutic potential of PI3Kγ inhibition, we required a potent and PI3Kγ-selective tool compound with sufficient metabolic stability for use in future in vivo studies. Herein, we describe some of our efforts to realize this goal through the systematic study of SARs within a series of 7-azaindole-based PI3Kγ inhibitors. The large volume of data generated from this study helped guide our subsequent lead optimization efforts and will inform further development of PI3Kγ-selective inhibitors for use in immunomodulation.

ACS Medicinal Chemistry Letters published new progress about 757978-19-1. 757978-19-1 belongs to iodides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Bromide,Iodide,Sulfamide,Benzene, name is 5-Bromo-3-iodo-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine, and the molecular formula is C13H8BrIN2O2S, Category: iodides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Yang, Chengbin published the artcileDevelopment of anti-breast cancer PI3K inhibitors based on 7-azaindole derivatives through scaffold hopping: Design, synthesis and in vitro biological evaluation, Application of 5-Bromo-3-iodo-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine, the publication is Bioorganic Chemistry (2021), 105405, database is CAplus and MEDLINE.

Breast cancer is the cancer with the highest incidence all over the world. Phosphatidylinositol 3-kinase is an important regulator of intracellular signaling pathways, which is frequently mutated and overexpressed in majority of human breast cancers, and the inhibition of PI3K has been considered as a promising approach for the treatment of the cancer. Here, we report our design and synthesis of new 7-azaindole derivatives as PI3K inhibitors through the scaffold hopping strategy. By varying the groups at the 3-position of 7-azaindole, we identified a series of potent PI3K inhibitors, whose antiproliferative activities against two human breast cancer MCF-7 and MDA-MB-231 cell lines were evaluated. Representative derivatives FD2054 and FD2078 showed better activity than BKM120 in antiproliferation, reduced the levels of phospho-AKT and induced cell apoptosis. All these results suggested that FD2054 and FD2078 are potent PI3K inhibitors that could be considered as potential candidates for the development of anticancer agents.

Bioorganic Chemistry published new progress about 757978-19-1. 757978-19-1 belongs to iodides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Bromide,Iodide,Sulfamide,Benzene, name is 5-Bromo-3-iodo-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine, and the molecular formula is C7H7IN2O, Application of 5-Bromo-3-iodo-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine.

Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Yang, Chengbin published the artcileDevelopment of anti-breast cancer PI3K inhibitors based on 7-azaindole derivatives through scaffold hopping: Design, synthesis and in vitro biological evaluation, Application of 5-Bromo-3-iodo-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine, the publication is Bioorganic Chemistry (2021), 105405, database is CAplus and MEDLINE.

Breast cancer is the cancer with the highest incidence all over the world. Phosphatidylinositol 3-kinase is an important regulator of intracellular signaling pathways, which is frequently mutated and overexpressed in majority of human breast cancers, and the inhibition of PI3K has been considered as a promising approach for the treatment of the cancer. Here, we report our design and synthesis of new 7-azaindole derivatives as PI3K inhibitors through the scaffold hopping strategy. By varying the groups at the 3-position of 7-azaindole, we identified a series of potent PI3K inhibitors, whose antiproliferative activities against two human breast cancer MCF-7 and MDA-MB-231 cell lines were evaluated. Representative derivatives FD2054 and FD2078 showed better activity than BKM120 in antiproliferation, reduced the levels of phospho-AKT and induced cell apoptosis. All these results suggested that FD2054 and FD2078 are potent PI3K inhibitors that could be considered as potential candidates for the development of anticancer agents.

Bioorganic Chemistry published new progress about 757978-19-1. 757978-19-1 belongs to iodides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Bromide,Iodide,Sulfamide,Benzene, name is 5-Bromo-3-iodo-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine, and the molecular formula is C7H7IN2O, Application of 5-Bromo-3-iodo-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine.

Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Lee, Soyoung published the artcileDevelopment and Biological Evaluation of Potent and Selective c-KIT^D816V Inhibitors, Quality Control of 757978-19-1, the publication is Journal of Medicinal Chemistry (2014), 57(15), 6428-6443, database is CAplus and MEDLINE.

The c-KIT tyrosine kinase has emerged as a potential therapeutic target for an array of diseases. However, there exists a drug resistance that is caused by mutations in c-KIT; therefore, c-KIT remains as a clin. challenge due to limited effective treatment options for therapies. For example, the acquired activating point mutation D816V significantly impairs the efficacy of targeted cancer therapies. Understanding the mechanisms of drug resistance at the mol. level will aid in designing and developing particular inhibitors with the potential to overcome these resistance mutations. The authors undertake a structure-based de novo design of 7-azaindole as the mol. core using the modified scoring function. This approach led to an identification of new c-KIT inhibitors over 100-fold specific for the D816V mutant relative to the wild-type c-KIT with nanomolar inhibitory activity. More importantly, these compounds potently inhibit clin. relevant D816V mutations of c-KIT in biochem. and cellular studies.

Journal of Medicinal Chemistry published new progress about 757978-19-1. 757978-19-1 belongs to iodides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Bromide,Iodide,Sulfamide,Benzene, name is 5-Bromo-3-iodo-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine, and the molecular formula is C13H8BrIN2O2S, Quality Control of 757978-19-1.

Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Hong, Seunghee published the artcileDiscovery of new azaindole-based PI3Kα inhibitors: Apoptotic and antiangiogenic effect on cancer cells, Formula: C13H8BrIN2O2S, the publication is Bioorganic & Medicinal Chemistry Letters (2010), 20(24), 7212-7215, database is CAplus and MEDLINE.

Phosphatidylinositol-3-kinase alpha (PI3Kα) is an important target in cancer due to the deregulation of the PI3K/AKT signaling pathway in many tumors. In this study, we designed [3,5-d]-7-azaindole analogs as PI3Kα inhibitors through the fragment-growing strategy. By varying groups at the 3,5-positions of azaindole, we developed the SAR (Structure-activity relationship) and identified a series of potent PI3Kα inhibitors. Representative azaindole derivatives showed activity in a cellular proliferation and apoptosis assays. Moreover, I exhibited strong antiangiogenic effects on cancer cells.

Bioorganic & Medicinal Chemistry Letters published new progress about 757978-19-1. 757978-19-1 belongs to iodides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Bromide,Iodide,Sulfamide,Benzene, name is 5-Bromo-3-iodo-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine, and the molecular formula is C13H8BrIN2O2S, Formula: C13H8BrIN2O2S.

Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Park, Hwangseo published the artcileStructure-based de novo design and identification of D816V mutant-selective c-KIT inhibitors, SDS of cas: 757978-19-1, the publication is Organic & Biomolecular Chemistry (2014), 12(26), 4644-4655, database is CAplus and MEDLINE.

To identify potent and selective inhibitors of D816V, the most common gain-of-function c-KIT mutant, the authors carried out structure-based de novo design using 7-azaindole as the core and the scoring function improved by implementing an accurate solvation free energy term. This approach led to the identification of new c-KIT inhibitors specific for the D816V mutant. The 3-(3,4-dimethoxyphenyl)-7-azaindole scaffold was optimized and represents a lead structure for the design of the potent and specific inhibitors of the D816V mutant. The results of mol. dynamics simulations indicate that hydrogen bonding interactions between the 7-azadindole moiety and the backbone groups of Cys673 are the most significant determinant for the potency and selectivity of c-KIT inhibitors.

Organic & Biomolecular Chemistry published new progress about 757978-19-1. 757978-19-1 belongs to iodides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Bromide,Iodide,Sulfamide,Benzene, name is 5-Bromo-3-iodo-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine, and the molecular formula is C13H8BrIN2O2S, SDS of cas: 757978-19-1.

Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Hong, Seunghee published the artcileDesign, Synthesis, and Evaluation of 3,5-Disubstituted 7-Azaindoles as Trk Inhibitors with Anticancer and Antiangiogenic Activities, Synthetic Route of 757978-19-1, the publication is Journal of Medicinal Chemistry (2012), 55(11), 5337-5349, database is CAplus and MEDLINE.

Tropomyosin-related kinase A (TrkA) is considered a promising target in the development of a therapeutic treatment of cancer and pain. Thus, a series of novel 7-azaindole-based Trk kinase inhibitors, e. g. I, were designed and synthesized through the structure-based design strategy. By varying the functional groups at the 3 and 5 positions of a 7-azaindole scaffold, the structure-activity relationships (SAR) profiles were explored and a series of potent Trk inhibitors were identified. Representative derivatives, including I, showed desirable activity in cellular proliferation and apoptosis assays. Moreover, these inhibitors exhibited noteworthy antiangiogenic activity.

Journal of Medicinal Chemistry published new progress about 757978-19-1. 757978-19-1 belongs to iodides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Bromide,Iodide,Sulfamide,Benzene, name is 5-Bromo-3-iodo-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine, and the molecular formula is C13H8BrIN2O2S, Synthetic Route of 757978-19-1.

Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com