Potent anti-prostate cancer agents derived from a novel androgen receptor down-regulating agent

Roles for the Backdoor Pathway of Androgen Metabolism in Prostate Cancer Response to Castration and Drug Treatment

“…TOK-001 was tolerated well and demonstrated anti-tumor activity. Purushottamachar et al provided evidence that TOK-001 not only inhibits CYP17A1 activity but has AR antagonistic capabilities similar to bicalutamide 47, 58. TAK-700 was designed to inhibit specifically the 18,20-lyase activity of CYP17A1, which focused the drug to target specifically adrenal androgen synthesis.…”

Antineoplastic Isoflavonoids Derived from Intermediate ortho‐Quinone Methides Generated from Mannich Bases

“…[1] Although the steroidal drug, abiraterone, interferes with the metabolism of adrenal androgens to testosterone and 5α-dihydrotestosterone by inhibiting cytochrome 17A1 (CYP17A1),[2] its effects are only short-lived when used after the failure of androgen-deprivation therapy. [3] Prostate cancer remains the second leading cause of cancer-related mortality in men,[4] and new therapies focused on the selective inhibition of enzymes participating in the backdoor pathway[5] to dihydrotestosterone from 4-androstene-3,17-dione remain a worthy goal for enhancing the extent or duration of response to androgen-deprivation therapy.…”

Synthesis, characterization and catalytic activity of Cu(II), Co(II), Ni(II), Mn(II) and Fe(III) complexes of 4-((3-formyl-4-hydroxyphenyl)diazenyl)-N-(4-methyloxazol-2-yl) benzenesulfonamide

“…Sulfonamide moiety has a vital functionality because of its wide varieties of reported biological [1,2] and pharmacological activities such as anticancer [3,4], carbonic anhydrase inhibitory [5,6], antibacterial [7,8], antimalarial [9], antitumor [10], antihypertensive [11], and anti-inflammatory [12]. Sulfonamide has been also reported to possess good herbicidal [13] and corrosion inhibitory properties [14,15].…”