Pyrazole-sulfonamide scaffold featuring dual-tail strategy as apoptosis inducers in colon cancer

Authors

Amira Khalil, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, The British University in Egypt (BUE), El Sherouk City 11837, Egypt.Follow
Reham M. M. El Hazek, Drug Radiation Research, National Center for Radiation Research & Technology (NCRRT), Egyptian Atomic Energy Authority, Cairo, Egypt
Nashwa H. Zaher, Drug Radiation Research, National Center for Radiation Research & Technology (NCRRT), Egyptian Atomic Energy Authority, Cairo, Egypt
Hagar E. S. Emam, Biomedical Research Division, Nawah Scientific, Cairo, Egypt
Marwa G. Elgazzar, Drug Radiation Research, National Center for Radiation Research & Technology (NCRRT), Egyptian Atomic Energy Authority, Cairo, Egypt

Document Type

Article

Publication Date

Spring 4-8-2023

Abstract

Dual-tail strategy has been successfully utilized in the development of novel carbonic anhydrase IX (CA IX) inhibitors. Herein we adopted this approach in the design and synthesis of a series of novel pyridine sulfonamide-pyrazole hybrid scaffold mimicking dual-tail inhibitors of CA IX. A library of 15 compounds was synthesized and assessed for their potential cytotoxic effects against colorectal cancer cells. Compounds 3, and 11 induced potential cytotoxic effects against the three cancer cell lines (HCT-116, HT-29, and SW-620) with IC₅₀s’ of 45.88, 28.27, and 16.57 uM, 25.01, 8.99, and 3.27 µM, respectively. Both compounds induced cellular apoptosis on HCT-116 and SW-620 cells, while compound 3 induced necrosis as well. In addition, both compounds induced cell cycle arrest on G0/G1, and S phases. Also, compound 11 showed potential autophagy induction on both colon cancer cell lines (HCT-116, and …

Recommended Citation

Khalil, Amira; El Hazek, Reham M. M.; Zaher, Nashwa H.; Emam, Hagar E. S.; and Elgazzar, Marwa G., "Pyrazole-sulfonamide scaffold featuring dual-tail strategy as apoptosis inducers in colon cancer" (2023). Pharmacy. 606.
https://buescholar.bue.edu.eg/pharmacy/606