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Article

Synthesis, Characterization, and Anticancer Activity of Benzothiazole Aniline Derivatives and Their Platinum (II) Complexes as New Chemotherapy Agents

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Institute of Biomedical Engineering Research, Kyungpook National University, 680, Gukchaebosang-ro, Jung-gu, Daegu 41944, Korea
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Department of Medical & Biological Engineering, Kyungpook National University, 80, Daehak-ro, Buk-gu, Daegu 41566, Korea
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R&D Center, Mirae BioPharm. Co., 124, Sagimakgol-ro, Jungwon-gu, Seongnam-si 13207, Korea
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InCerebro Drug Discovery Institute, Seoul 01811, Korea
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Department of Biomedical Science, School of Medicine, Kyungpook National University, 680, Gukchaebosang-ro, Jung-gu, Daegu 41944, Korea
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Department of Chemistry, Kyungpook National University, 80, Daehak-ro, Buk-gu, Daegu 41566, Korea
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Laboratory Animal Center, the Daegu-Gyeongbuk Medical Innovation Foundation, 88 Dongnae-ro, Dong-gu, Daegu 41061, Korea
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Department of Molecular Medicine, School of Medicine, Kyungpook National University, 680, Gukchaebosang-ro, Jung-gu, Daegu 41944, Korea
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Department of Radiology, Kyungpook National University Hospital, 130 Dongdeok-ro, Jung-gu, Daegu 41944, Korea
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Authors to whom correspondence should be addressed.
Academic Editor: Luís M. T. Frija
Pharmaceuticals 2021, 14(8), 832; https://0-doi-org.brum.beds.ac.uk/10.3390/ph14080832
Received: 30 July 2021 / Revised: 19 August 2021 / Accepted: 21 August 2021 / Published: 23 August 2021
(This article belongs to the Special Issue Selective Chelators for Metals on Cells and Cancer Chemotherapy)
We describe the synthesis, characterization, molecular modeling, and in vitro anticancer activity of three benzothiazole aniline (BTA) ligands and their corresponding platinum (II) complexes. We designed the compounds based on the selective antitumor properties of BTA, along with three types of metallic centers, aiming to take advantage of the distinctive and synergistic activity of the complexes to develop anticancer agents. The compounds were characterized using nuclear magnetic resonance spectrometry, Fourier transform infrared spectroscopy, mass spectrometry, elemental analysis, and tested for antiproliferative activity against multiple normal and cancerous cell lines. L1, L2, and L1Pt had better cytotoxicity in the liver, breast, lung, prostate, kidney, and brain cells than clinically used cisplatin. Especially, L1 and L1Pt demonstrated selective inhibitory activities against liver cancer cells. Therefore, these compounds can be a promising alternative to the present chemotherapy drugs. View Full-Text
Keywords: benzothiazole aniline (BTA); platinum (II); anticancer; DNA; liver; docking benzothiazole aniline (BTA); platinum (II); anticancer; DNA; liver; docking
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MDPI and ACS Style

Islam, M.K.; Baek, A.-R.; Sung, B.; Yang, B.-W.; Choi, G.; Park, H.-J.; Kim, Y.-H.; Kim, M.; Ha, S.; Lee, G.-H.; Kim, H.-K.; Chang, Y. Synthesis, Characterization, and Anticancer Activity of Benzothiazole Aniline Derivatives and Their Platinum (II) Complexes as New Chemotherapy Agents. Pharmaceuticals 2021, 14, 832. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14080832

AMA Style

Islam MK, Baek A-R, Sung B, Yang B-W, Choi G, Park H-J, Kim Y-H, Kim M, Ha S, Lee G-H, Kim H-K, Chang Y. Synthesis, Characterization, and Anticancer Activity of Benzothiazole Aniline Derivatives and Their Platinum (II) Complexes as New Chemotherapy Agents. Pharmaceuticals. 2021; 14(8):832. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14080832

Chicago/Turabian Style

Islam, Md. K., Ah-Rum Baek, Bokyung Sung, Byeong-Woo Yang, Garam Choi, Hyun-Jin Park, Yeoun-Hee Kim, Minsup Kim, Seongmin Ha, Gang-Ho Lee, Hee-Kyung Kim, and Yongmin Chang. 2021. "Synthesis, Characterization, and Anticancer Activity of Benzothiazole Aniline Derivatives and Their Platinum (II) Complexes as New Chemotherapy Agents" Pharmaceuticals 14, no. 8: 832. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14080832

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