Medicinal Chemistry

Synthesis and Evaluation of 5-Chloro-2-Methoxy-N-(4-Sulphamoylphenyl) Benzamide Derivatives as Anti-cancer Agents

Abstract

Ahmed M Abdelaziz, Mingfeng Yu, Peng Li, Longjin Zhong, Abdel Nasser B Singab, Atef G Hanna, Khaled A Abouzid, Maged KG Mekhael and Shudong Wang

Sulphonamides embrace a sublime class of drugs with various biological activities. Since the discovery of E7010 in 1992, several sulphonamides as anti-cancer drug candidates have been identified. Herein, a new series of 5-chloro- 2-methoxy-N-(4-sulphamoylphenyl)benzamide derivatives was synthesised, and their anti-proliferative activity was evaluated against human ovarian cancer (A2780) and colon cancer (HCT-116) cell lines. As one of the most potent antiproliferative agents, compound 4j was further tested against a panel of cancer cell lines revealing that human pancreatic carcinoma (MIA PaCa-2) displayed the highest sensitivity. Cellular mechanistic studies on MIA PaCa-2 cells showed that 4j arrested the G2/M cell cycle and induced apoptosis.