title: Synthesis of New 3-Heteroarylindoles as Potential Anticancer Agents.
abstract: 2-(3-(1H-Indol-3-yl)-5-(p-tolyl)-4,5-dihydro-1H-pyrazol-1-yl)-4-substituted-5-(substituted diazenyl)thiazoles and 2-(1H-indol-3-yl)-9-substituted-4,7-disubstituted pyrido[3,2-e][1,2,4]triazolo[4,3-a]pyrimidin-5(7H)-ones were synthesized via reaction of hydrazonoyl halides with each of 3-(1H-indol-2-yl)-5-(p-tolyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide and 7-(1H-indol-3-yl)-2- thioxo-5-substituted-2,3-dihydropyrido[2,3-d]pyrimidin-4(1H)-ones, respectively. Also, hydrazonoyl halides were reacted with N'-(1-(1H-indol-3-yl)ethylidene)-2-cyanoacetohydrazide to afford 1,3,4-thiadiazole derivatives. Structures of the new synthesis were elucidated on the basis of elemental analysis, spectral data, and alternative synthetic routes whenever possible. Fifteen of the new compounds have been evaluated for their antitumor activity against the MCF-7 human breast carcinoma cell line. The results indicated that many of the tested compounds showed moderate to high anticancer activity when compared with doxorubicin as a reference drug.
authors.affiliation: Department of Chemistry, Faculty of Science, Cairo University, Giza 12613, Egypt. abdelhamid45@gmail.com.
authors.forename: Abdou O
authors.initials: AO
authors.lastname: Abdelhamid
authors.affiliation: Department of Chemistry, Faculty of Science, Cairo University, Giza 12613, Egypt. s.m.gomha@gmail.com.
authors.forename: Sobhi M
authors.initials: SM
authors.lastname: Gomha
authors.affiliation: Department of Chemistry, Faculty of Science, Cairo University, Giza 12613, Egypt. nadia.abdelhamid5@gmail.com.
authors.forename: Nadia A
authors.initials: NA
authors.lastname: Abdelriheem
authors.affiliation: Chemistry of Natural Compounds, Department National Research Center, Dokki 12622, Egypt. SaherKamel@yahoo.com.
authors.forename: Saher M
authors.initials: SM
authors.lastname: Kandeel
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D013844:Thiazoles / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D007211:Indoles; D013844:Thiazoles
keywords: anti-cancer activity; coupling reactions; molecular docking; pyrazoles; thiazoles; thiosemicarbazides