N-Acylated and N, N′-diacylated imidazolidine-2-thione derivatives and N, N′-diacylated tetrahydropyrimidine-2(1 H)-thione analogues: Synthesis and antiproliferative activity

Fifty-one acylthioureas (ATUs) incorporating imidazolidine-2-thione or its upper cyclohomologue were prepared by parallel synthesis and evaluated against a high number of human cancer cell lines for antiproliferative activity. ATUs 1o (3,5-dichlorobenzoyl), 1s (2-furoyl), 3s (2-furoyl) and 1t (2-thenoyl) displayed activity against leukemia, melanoma LOX IMVI, non-small cell lung NCI-H522, renal 786-0, CAKI-1, SN12C, UO-31 and breast MCF7, MDA-MB-435, T-47D cancer cell lines in the 0.3–9.7 μM concentration range. Compound 14s exhibited selectivity for melanoma SK-MEL-5 (GI 50 < 5 nM); 1s for leukemia MOLT-4 (GI 50: 300 nM); 1q, 3b and 3q for renal cancer UO-31 (GI 50: 70–200 nM); 8s, 9s for non-small cell lung cancer EKVX (GI 50: 300, 10 nM) and 3j for HOP-92 (GI 50: 700 nM) cell line. [Display omitted]