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.
Highlights
Cancer poses a serious human health problem despite much progress in understanding its biology and pharmacology
The starting material 1 was synthesized according to the reported literature [29] (Scheme 1)
The starting material 1 was used to synthesize the 3-amino-4-cyanopyrazolo derivative 2 which was treated with formamide or hydrazine hydrate to afford the corresponding aminopyrazolopyrimidine 3 and aminopyrazolopyrazole derivative 4, respectively
Summary
Cancer poses a serious human health problem despite much progress in understanding its biology and pharmacology. These derivatives are well known for their pronounced inhibition of the growth of cytomegalovirus (HCMV)-human cytomegalovirus [4], and are used as corticotrophin-releasing hormone (CRH-R1) receptor antagonists (display antidepressant activity) [5]. Pyrimidine derivatives are used as Tie-2 kinase inhibitors [13,14], Human immunodeficiency virus type-1 (HIV-1) inhibitors [15,16], antimalarials [17,18], adenosine A1 receptor antagonists [19], anticancer agents [20], analgesics [21], cardiovascular [22]. Are primarily contributed by the presence of heterocyclic rings in their molecular make-up In view of these reports and in continuation of our previous works in heterocyclic chemistry, we report here newly synthesized substituted pyrazole derivatives. The androgen receptor antagonist, and anti-prostate cancer activities for the synthesized compounds was evaluated using Bicalutamide as a reference drug
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