Bioorganic Chemistry 93 (2019) ii-xviii Contents lists available at ScienceDirect Bioorganic Chemistry journal homepage: www.elsevier.com/locate/bioorg Graphical Abstracts/Bioorganic Chemistry 93 (2019) ii-xviii REGULAR ARTICLES Aminonaphthalimide hybrids of mitoxantrone and amonafide as anticancer and fluorescent Bioorganic Chemistry 93 (2019) 103287 cellular imaging agents Alex D. Johnsona, Rodrianne Zammitb, Jasmine Vellac, Mario Valentinoc, Joseph A. Buhagiarb, David C. Magria aDepartment of Chemistry, Faculty of Science, University of Malta, Msida, MSD 2080, Malta bDepartment of Biology, Faculty of Science, University of Malta, Msida, MSD 2080, Malta cDepartment of Physiology and Biochemistry, Faculty of Medicine & Surgery, University of Malta, Msida, MSD 2080, Malta Adapalene inhibits ovarian cancer ES-2 cells growth by Bioorganic Chemistry 93 (2019) 103315 targeting glutamic-oxaloacetic transaminase 1 Qiqi Wangb, Qingzhe Zhanga, Shanshan Luana, Kaiyin Yanga, Mengzhu Zhenga, Kezhen Lic, Lixia Chenb, Hua Lia aHubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China bWuya College of Innovation, Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China cCancer Biology Center, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China Synthesis of novel nitroreductase enzyme-activated nitric oxide Bioorganic Chemistry 93 (2019) 103318 prodrugs to site-specifically kill bacteria Hailey A.J. Hibbarda, Melissa M. Reynoldsa,b aDepartment of Chemistry, Colorado State University, Fort Collins, CO 80523, USA bSchool of Biomedical Engineering, Colorado State University, Fort Collins, CO 80523, USA Graphical Abstracts Design and synthesis of substituted Bioorganic Chemistry 93 (2019) 103317 dihydropyrimidinone derivatives as cytotoxic and tubulin polymerization inhibitors Sravani Sanaa, Ramya Tokalaa, Deepti Madanlal Bajajb, Narayana Nageshd, Kiran Kumar Bokarad, Gaddam Kiranmaid, Uppu Jaya Lakshmia, Swapna Vadlamanic, Venu Tallab, Nagula Shankaraiaha aDepartment of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500 037, India bDepartment of Pharmacology and Toxicology, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500 037, India cDepartment of Pharmaceutical Technology in Process Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500 037, India dCSIR-Centre for Cellular and Molecular Biology, Medical Biotechnology Complex, ANNEXE II, Uppal Road, Uppal, Hyderabad 500007, India Synthesis and anti-tyrosinase mechanism of the substituted vanillyl cinnamate analogues Bioorganic Chemistry 93 (2019) 103316 Zefeng Zhaoa, Guangxin Liub, Yufeng Menga, Jiale Tiana, Xufei Chena, Meilun Shenb, Yuexuan Lia, Bingyao Lia, Cong Gaoa, Shaoping Wua, Cuiqin Lib, Xirui Hec, Ru Jiangd, Mingcheng Qiane,f, Xiaohui Zhenga aSchool of Pharmacy, Biomedicine Key Laboratory of Shaanxi Province, Northwest University, Xi’an, China bKey Laboratory of the Ministry of Education for Medicinal Resources and Natural Pharmaceutical Chemistry, National Engineering Laboratory for Resource Development of Endangered Crude Drugs in Northwest of China, College of Life Sciences, Shaanxi Normal University, Xi’an, Shaanxi, China cDepartment of Bioengineering, Zhuhai Campus of Zunyi Medical University, Zhuhai, 519041, China dSchool of Pharmacy, The Fourth Military Medical University, Xi’an, Shaanxi, China eDepartment of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou 213164, Jiangsu, China fLaboratory for Medicinal Chemistry, Ghent University, Ottergemsesteenweg 460, B-9000 Ghent, Belgium Design, synthesis and preliminary in-vitro studies of novel boronated monocarbonyl Bioorganic Chemistry 93 (2019) 103324 analogues of Curcumin (BMAC) for antitumor and ß-amiloyd disaggregation activity Emanuele Azzia, Diego Albertib, Stefano Parisottoa, Alberto Oppedisanoa, Nicoletta Prottic,d, Saverio Altieric,d, Simonetta Geninatti-Crichb, Annamaria Deagostinoa aDepartment of Chemistry, University of Turin, via P. Giuria 7, 10125 Turin, Italy bDepartment of Molecular Biotechnology and Health Sciences, University of Turin, via Nizza 52, 10126 Turin, Italy cDepartment of Physics, University of Pavia, via Agostino Bassi 6, Pavia 27100, Italy dNuclear Physics National Institute (INFN), Unit of Pavia, via Agostino Bassi 6, Pavia 27100, Italy Design, synthesis and biological evaluation of novel copper- Bioorganic Chemistry 93 (2019) 103322 chelating acetylcholinesterase inhibitors with pyridine and N-benzylpiperidine fragments Yeheng Zhoua,d, Wei Suna, Jiale Pengd, Hui Yana, Li Zhangd, Xingyong Liud, Zhili Zuoa,b,c,d aState Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, PR China bYunnan Key Laboratory of Natural Medicinal Chemistry, Kunming 650201, PR China cUniversity of Chinese Academy of Sciences, Beijing 100049, PR China dSchool of Chemical Engineering, Sichuan University of Science & Engineering, Zigong 643000, PR China iii Graphical Abstracts Design, synthesis and biological evaluation of some new 1,3,4-thiadiazine-thiourea Bioorganic Chemistry 93 (2019) 103323 derivatives as potential antitumor agents against non-small cell lung cancer cells Synthesis of some thiadiazine-thiourea derivative 5a-p Fatma A.F. Ragaba, Salah A. Abdel-Azizb, Marwa Kamelc, Abdelsalam Mohamed A. Oufb, Cytotoxicity assay against NSCLC Heba Abdelrasheed Allama 5d, 5i, 5j most potent compounds aDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo P.O. Box, 11562, Egypt 5i bDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, Assiut 71524, Egypt 5d 5j cDepartment of Cancer Biology, Unit of Pharmacology, National Cancer Institute, Cairo University, Egypt Biological assessment VEGFR2 B-RAF MMP9 Selectivity index against WI-38 Further evaluation for 5j (most promising) Cell cycle analysis Apoptosis Invasion and migration assays Docking 5d,5i, 5j are potenƟaů targeƟng agents against NSCLC Identification of a potent and selective gametocytocidal Bioorganic Chemistry 93 (2019) 103321 antimalarial agent from the stem barks of Lophira lanceolata Annalisa Lopatrielloa, Harouna Soréb, Annette Habluetzelc, Silvia Parapinid, Sarah D'Alessandrod, Donatella Taramellie, Orazio Taglialatela-Scafatia aDepartment of Pharmacy, School of Medicine and Surgery, University of Naples Federico II, Via D. Montesano 49, 80131 Naples, Italy bCentre National de Recherche et de Formation sur le Paludisme, 01 BP 2208 Ouagadougou, Burkina Faso cSchool of Pharmacy, University of Camerino, Via Madonna delle Carceri 9, 62032 Camerino, Italy dDepartment of Biomedical, Surgical and Dental Sciences, Università degli Studi di Milano, Via Pascal 36, 20133 Milano, Italy eDepartment of Pharmacological and Biomolecular Sciences, Università degli Studi di Milano, Via Pascal 36, 20133 Milano, Italy Design, synthesis and biological evaluation of resveratrol-cinnamoyl derivates Bioorganic Chemistry 93 (2019) 103319 as tubulin polymerization inhibitors targeting the colchicine binding site Yong Yin, Bao-Ping Lian, Yuan-Zheng Xia, Yu-Ying Shao, Ling-Yi Kong Jiangsu Key Laboratory of Bioactive Natural Product Research and State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, School of Traditional Chinese Pharmacy, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, People’s Republic of China Exploration of Pd-catalysed four-component tandem reaction for one-pot Bioorganic Chemistry 93 (2019) 103314 assembly of pyrazolo[1,5-c]quinazolines as potential EGFR inhibitors Arshad J. Ansaria, Gaurav Joshib, Umesh Prasad Yadavc, Antim K. Mauryad, Vijai K. Agnihotrid, Sourav Kalrac, Raj Kumarb, Sandeep Singhc, Devesh M. Sawanta aSchool of Chemical Sciences and Pharmacy, Central University of Rajasthan NH-8, Bandarsindri, Ajmer 305817, Raj, India bLaboratory for Drug Design and Synthesis, Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Bathinda 151001, Punjab, India cLaboratory of Molecular Medicine, Department of Human Genetics and Molecular Medicine, Central University of Punjab, Bathinda 151001, Punjab, India dNatural Product Chemistry and Process Development Division, CSIR-IHBT, Palampur, Himachal Pradesh 176061, India iv Graphical Abstracts Novel tribenzylaminobenzolsulphonylimine based Bioorganic Chemistry 93 (2019) 103313 on their pyrazine and pyridazines: Synthesis, characterization, antidiabetic, anticancer, anticholinergic, and molecular docking studies Gulnar Mamedovaa, Adila Mahmudovaa, Sabir Mamedova, Yavuz Erdenb, Parham Taslimic, Burak Tüzünd, Recep Tasc, Vagif Farzaliyeva, Afsun Sujayeva, Saleh H. Alwasele, Ilhami Gulçinf aLaboratory of Faine Organic Synthesis, Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences, 1029 Baku, Azerbaijan bDepartment of Molecular Biology and Genetics, Faculty of Science, Bartin University, 74100 Bartin, Turkey cDepartment of Biotechnology, Faculty of Science, Bartin University, 74100 Bartin, Turkey dDepartment of Chemistry, Faculty of Science, Cumhuriyet University, 58140 Sivas, Turkey eDepartment of Zoology,