Synthesis and anticancer activity evaluation of some hemin and hematoporphyrin derivatives

388-393Sulphamerazine, sulphadiazine, and sulphaguanidine are coupled with hemin to give bis coupled products 1a, 1b and 1c respectively. 3, 4-Diphenyliminothiazoline, sulphamerazine, sulphaacetamide, sulphathiazole and sulphadiazine on coupling with hematoporphyrin give bis coupled products 2a, 2b, 2c, 2d and 2e respectively. Compounds 1a-c and 2a-e have been screened for anticancer activity against a small panel of six cancer cell lines consisting of prostate(DU 145), colon (HT29), melanoma (LOX), breast(MCF7 and MCF7/ADR) and CNS(U251) tumors. Best GI50 (concentration which inhibits the cell growth by 50%) values are shown by 2c, 2.2μM(prostate tumor, cell line DU145); 2c 13.0μM(colon tumor, cell line HT29); 2b, 3.4μM(melanoma tumor, cell line LOX); 2c, 9.7μM(breast tumor, cell line MCF7); 2a, 3.1μM(breast, tumor, cell line MCF7/ADR) and 1c, 3.4μM(CNS tumor, cell line U251) respectively. Out of all the compounds reported here GI50 value shown by 2a i.e.3.1μM against breast, tumor (MCF7/ADR) is quite close to the GI50 value i.e. 1.8μM, of standard drug doxorubicin