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Development of 2-mercaptobenzamides as small molecule inhibitors of HIV maturation

Thursday, September 15, 2016 — Poster Session II

12:00 p.m. – 1:30 p.m.
FAES Terrace
NIDDK
CHEMBIO-7

Authors

  • M Saha
  • MT Scerba
  • DH Appella

Abstract

HIV-1 nucleocapsid protein 7 (NCp7), a zinc finger protein, is an attractive target for antiretroviral drugs due to its essential role in viral replication and maturation. We envision that the development of zinc finger inhibitors targeting the highly conserved, mutation-resistant NCp7 will serve as a welcomed addition in the fight against HIV. Herein, we report a series of 2-mercaptobenzamide prodrugs that target the NCp7 domain of HIV-1. Our preliminary data showed that the 2-mercaptobenzamide prodrugs inhibit virus-induced cell lysis in CEM-SS cells with EC50 values of 1-100 µM. Notably, cell viability studies in the same cell line indicate that these molecules are also non-toxic (TC50>100 µM). These prodrugs are easily synthesized in two steps from inexpensive starting materials.

Category: Chemical Biology