Browsing by Author "Algso, Muheb"

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Design and Synthesis of Novel Thieno-Dibenzothiophene Derivatives
(Amer Chemical Soc, 2017) Kivrak, Arif; Algso, Muheb
Synthesis and Biological Activity of New Indole Based Derivatives as Potent Anticancer, Antioxidant and Antimicrobial Agents
(Elsevier, 2022) Konus, Metin; Cetin, Dogan; Kizilkan, Nurhan Didem; Yilmaz, Can; Fidan, Ceylan; Algso, Muheb; Arslan, Sevki
Indoles have very critical roles to design new biologically active molecules in medicinal chemistry. They display higher biological activities or create new biological properties when compared to the other heteroaromatic compounds. In the present study, 1-ethyl-2-phenyl-3-(thiophen-2-yl)-1H-indole (3), 8-ethyl-8H-benzo[a]thieno[3,2-c]carbazole (4), 1-ethyl-2-phenyl-3-(5-(phenylethynyl)thiophen-2-yl)-1H-indole (6) and 1-ethyl-3-(furan-2-yl)-2-phenyl-1H-indole (7) are prepared via Pd-catalyzed cross-coupling reactions and iodocyclization reactions. It was determined that compound 3 and 7 were also seemed to be better drug candidates at the end of in silico evaluation. Furthermore, compound 7 provided the best antibacterial and antifungal activity against the test indicator strains. It showed a potent antifungal effect on Aspergillus niger ATCC 16404 (MIC: 1.17 mu g mL(-1); MFC: 2.7 mu g mL(-1)). In addition, while compounds 3, 6 and 7 showed significantly high molybdenum reducing activity compared to trolox, 7 exhibited almost the same antioxidant activity (EC50 = 7.1 mu M) compared to the trolox standard (EC50 = 5.07 mu M). After characterization, the cytotoxic activities of novel indoles were tested against different cancer cell lines and non-cancerous human cell line. Compound 3 and 7 had selective cytotoxic activity towards cancer cells. EC50 values of compound 3 were found to be 248.15 mu M for LnCap, 139.81 mu M for HepG2, and 164.72 mu M for the Caco-2 cell line. Similarly, The EC50 value of 7 was found as 38.725 mu M for LnCap, 70.02 mu M for HepG2, and 86.98 mu M for Caco-2, and 90.97 mu M for Hek293 cell line. Moreover, it was revealed that these two compounds showed strong apoptotic properties towards these cancer cell lines as described by image cytometry and real time PCR. Consequently, these results improved that our molecules 3 and 7 could be new candidates as anticancer agents and apoptosis inducers. (C) 2022 Elsevier B.V. All rights reserved.
Synthesis of Ethynyl-Thiophene Derivatives, Antioxidant Properties and Adme Analysis
(Wiley-v C H verlag Gmbh, 2022) Konus, Metin; Algso, Muheb; Yilmaz, Can; Khorsheed, Bahzad Ahmed; Koroglu, Asli; Cetin, Dogan; Kivrak, Arif
Herein, novel alkyne based organic compounds, 2-((2-(methylthio)phenyl)ethynyl)thiophene (MAT) and 2-ethynyl-3-(phenylethynyl)thiophene (DAT), were designed and synthesized via Pd-catalyst cross-coupling reactions. The isolated yields of MAT and DAT were obtained as 77 % and 96 %, respectively. After chemical characterization, radical scavenging activities and reduction power capacities of them were determined by DPPH, TEAC, phosphomolybdenum and reducing power methods. MAT showed higher radical scavenging activities than DAT, and comparable with the standard. Moreover, basic ADME properties were calculated in silico. Both of the newly synthesized derivatives were reported with the same moderate to good drug score of 0.42; and, having potential to pass through BBB and GI with no appointed toxic effects.