title: Inhibitors of apoptosis in testicular germ cells: synthesis and biological evaluation of some novel IBTs bearing sulfonamide moiety.
abstract: Pifithrin-α, a known p53 inactivator, inhibits p53-dependant mitochondrial cell death induced by toxins or γ-radiation. It has been found that aromatic IBT analogues of PFT-α are more cytoprotective and nonpeptide-based, isatin sulfonamides selectively inhibit caspases 3 and 7, responsible for mitochondrial mediated apoptosis. Therefore, we envisioned the synthesis of novel IBTs 4 and 5 bearing sulfonamide moiety and observed the mitigating effects of these IBTs in rescue of malathion induced apoptosis in testicular germ cells of goat. Two IBTs (4b; R = CH(3), 5b; R(1) = Cl) showed very high survival rate of cells whereas IBT 4f (R = NO(2)) showed some exceptional behaviour by increasing the apoptosis. These IBTs nullify the cytotoxic effect of malathion on mitochondria, following p53-independent pathway.
authors.affiliation: Department of Chemistry, Kurukshetra University, Kurukshetra 136119, Haryana, India.
authors.forename: Navneet
authors.initials: N
authors.lastname: Chandak
authors.forename: Jitender K
authors.initials: JK
authors.lastname: Bhardwaj
authors.forename: Rajnesh K
authors.initials: RK
authors.lastname: Sharma
authors.forename: Pawan K
authors.initials: PK
authors.lastname: Sharma
mesh_terms: D000818:Animals; D017209:Apoptosis / Q000187:drug effects*; D002470:Cell Survival / Q000187:drug effects; D005854:Germ Cells / Q000166:cytology / Q000187:drug effects*; D006041:Goats; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D008297:Male; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013737:Testis / Q000166:cytology*; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D007093:Imidazoles; D013449:Sulfonamides; D013844:Thiazoles