title: Androgen receptor antagonists and anti-prostate cancer activities of some newly synthesized substituted fused pyrazolo-, triazolo- and thiazolo-pyrimidine derivatives.
abstract: A series of substituted pyrazole, triazole and thiazole derivatives (2-13) were synthesized from 1-(naphtho[1,2-d]thiazol-2-yl)hydrazine as starting material and evaluated as androgen receptor antagonists and anti-prostate cancer agents. The newly synthesized compounds showed potent androgen receptor antagonists and anti-prostate cancer activities with low toxicity (lethal dose 50 (LD50)) comparable to Bicalutamide as reference drug. The structures of newly synthesized compounds were confirmed by IR, 1H-NMR, 13C-NMR, and MS spectral data and elemental analysis. The detailed synthesis, spectroscopic data, LD50 values and pharmacological activities of the synthesized compounds are reported.
authors.affiliation: Pharmacology and Toxicology Department, College of Pharmacy, Taibah University, Almadinah Almunawarah 22624, Saudi Arabia. drsalehamb@yahoo.com.
authors.forename: Saleh A
authors.initials: SA
authors.lastname: Bahashwan
authors.affiliation: Respiratory Therapy Department, College of Medical Rehabilitation Sciences, Taibah University, Almadina Almanoara 22624, Saudi Arabia. dr_ahmedfayed14@yahoo.com.
authors.forename: Ahmed A
authors.initials: AA
authors.lastname: Fayed
authors.affiliation: Microbiology and Immunology Departments, College of Medicine, Taibah University, Almadinah Almunawarah 22624, Saudi Arabia. mmostafa201120@yahoo.com.
authors.forename: Mohamed A
authors.initials: MA
authors.lastname: Ramadan
authors.affiliation: National Research Center, Cairo, Dokki 12622, Egypt. aeamr1963@yahoo.com.
authors.forename: Abd El-Galil E
authors.initials: Ael-G
authors.lastname: Amr
authors.affiliation: Pharmacology and Toxicology Department, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia. ouf.nabil@yahoo.com.
authors.forename: Naif O
authors.initials: NO
authors.lastname: Al-Harbi
mesh_terms: D059002:Androgen Receptor Antagonists / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D016466:CHO Cells; D002460:Cell Line; D045744:Cell Line, Tumor; D003412:Cricetulus; D006801:Humans; D007928:Lethal Dose 50; D008297:Male; D011471:Prostatic Neoplasms / Q000188:drug therapy*; D011720:Pyrazoles / Q000494:pharmacology*; D011743:Pyrimidines / Q000494:pharmacology*; D013844:Thiazoles / Q000494:pharmacology*; D014230:Triazoles / Q000494:pharmacology*
chemical_list: D059002:Androgen Receptor Antagonists; D000970:Antineoplastic Agents; D011720:Pyrazoles; D011743:Pyrimidines; D013844:Thiazoles; D014230:Triazoles; C031280:pyrazole