title: Synthesis and evaluation of novel 17-indazole androstene derivatives designed as CYP17 inhibitors.
abstract: A series of novel 1H- and 2H-indazole derivatives of the commercially available dehydroepiandrosterone acetate have been synthesized and tested for inhibition of human cytochrome 17alpha-hydroxylase-C(17,20)-lyase (CYP17), androgen receptor (AR) binding affinity, and cytotoxic potential against three prostate cancer (PC) cell lines.
authors: Laboratório de Química Farmacêutica, Faculdade de Farmácia, Universidade de Coimbra, Rua do Norte, 3000-295, Coimbra, Portugal.
authors: Vânia M A
authors: VM
authors: Moreira
authors: Tadas S
authors: TS
authors: Vasaitis
authors: Vincent C O
authors: VC
authors: Njar
authors: Jorge A R
authors: JA
authors: Salvador
mesh_terms: D001667:Binding, Competitive / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003687:Dehydroepiandrosterone / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D006801:Humans; D008297:Male; D011471:Prostatic Neoplasms / Q000201:enzymology / Q000473:pathology; D011944:Receptors, Androgen / Q000378:metabolism; D013254:Steroid 17-alpha-Hydroxylase / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D011944:Receptors, Androgen; D003687:Dehydroepiandrosterone; C028163:dehydroepiandrosterone acetate; D013254:Steroid 17-alpha-Hydroxylase