Design, synthesis and molecular modelling studies of some pyrazole derivatives as carbonic anhydrase inhibitors

by Yazgı Dizdaroglu, Canan Albay, Tayfun Arslan, Abdulilah Ece, Emir A. Turkoglu, Asiye Efe, Murat Senturk, Claudiu T. Supuran, Deniz Ekinci
Published 2020-01-01

Sulphonamides incorporating 1,3,5-triazine structural motifs show antioxidant, acetylcholinesterase, butyrylcholinesterase, and tyrosinase inhibitory profile

by Nabih Lolak, Mehmet Boga, Muhammed Tuneg, Gulcin Karakoc, Suleyman Akocak, Claudiu T. Supuran
Published 2020-01-01

Imidazothiazole-based potent inhibitors of V600E-B-RAF kinase with promising anti-melanoma activity: biological and computational studies

by Hanan S. Anbar, Mohammed I. El-Gamal, Hamadeh Tarazi, Bong S. Lee, Hong R. Jeon, Dow Kwon, Chang-Hyun Oh
Published 2020-01-01

In vivo antiaging effects of alkaline water supplementation

by Mariantonia Logozzi, Davide Mizzoni, Rossella Di Raimo, Mauro Andreotti, Daniele Macchia, Massimo Spada, Stefano Fais
Published 2020-01-01

Histidine residues at the copper-binding site in human tyrosinase are essential for its catalytic activities

by Hyangsoon Noh, Sung Jun Lee, Hyun-Joo Jo, Hye Won Choi, Sungguan Hong, Kwang-Hoon Kong
Published 2020-01-01

Synthesis, activity and mechanism of alkoxy-, carbamato-, sulfonamido-, thioureido-, and ureido-derivatives of 2,4,5-trimethylpyridin-3-ol against inflammatory bowel disease

by Chhabi Lal Chaudhary, Pallavi Gurung, Seoul Jang, Suhrid Banskota, Tae-Gyu Nam, Jung-Ae Kim, Byeong-Seon Jeong
Published 2020-01-01

Synthesis and biological evaluation of new 3(2H)-pyridazinone derivatives as non-toxic anti-proliferative compounds against human colon carcinoma HCT116 cells

by Zeynep Özdemir, Semra Utku, Bijo Mathew, Simone Carradori, Giustino Orlando, Simonetta Di Simone, Mehmet Abdullah Alagöz, Azime Berna Özçelik, Mehtap Uysal, Claudio Ferrante
Published 2020-01-01

Design, synthesis, molecular modelling and biological evaluation of novel 3-(2-naphthyl)-1-phenyl-1H-pyrazole derivatives as potent antioxidants and 15-Lipoxygenase inhibitors

by Sahar A. Ali, Samir Mohamed Awad, Ahmed Mohammed Said, Shahenda Mahgoub, Heba Taha, Naglaa Mohamed Ahmed
Published 2020-01-01

Design, synthesis and evaluation of quinolinone derivatives containing dithiocarbamate moiety as multifunctional AChE inhibitors for the treatment of Alzheimer’s disease

by Jie Fu, Fengqi Bao, Min Gu, Jing Liu, Zhipeng Zhang, Jiaoli Ding, Sai-Sai Xie, Jinsong Ding
Published 2020-01-01

Preparation, carbonic anhydrase enzyme inhibition and antioxidant activity of novel 7-amino-3,4-dihydroquinolin-2(1H)-one derivatives incorporating mono or dipeptide moiety

by Hasan Küçükbay, Zeynep Gönül, F. Zehra Küçükbay, Andrea Angeli, Gianluca Bartolucci, Claudiu T. Supuran
Published 2020-01-01

Novel insights on saccharin- and acesulfame-based carbonic anhydrase inhibitors: design, synthesis, modelling investigations and biological activity evaluation

by Paolo Guglielmi, Giulia Rotondi, Daniela Secci, Andrea Angeli, Paola Chimenti, Alessio Nocentini, Alessandro Bonardi, Paola Gratteri, Simone Carradori, Claudiu T. Supuran
Published 2020-01-01

Identification of probe-quality degraders for Poly(ADP-ribose) polymerase-1 (PARP-1)

by Zhimin Zhang, Xinyue Chang, Chixiao Zhang, Shenxin Zeng, Meihao Liang, Zhen Ma, Zunyuan Wang, Wenhai Huang, Zhengrong Shen
Published 2020-01-01

Examination of sulfonamide-based inhibitors of MMP3 using the conditioned media of invasive glioma cells

by Alisha T. Poole, Christopher A. Sitko, Caitlin Le, Christian C. Naus, Bryan M. Hill, Eric A. C. Bushnell, Vincent C. Chen
Published 2020-01-01

Design and synthesis of tricyclic terpenoid derivatives as novel PTP1B inhibitors with improved pharmacological property and in vivo antihyperglycaemic efficacy

by Lingling Yang, Feng Chen, Cheng Gao, Jiabao Chen, Junyan Li, Siyan Liu, Yuanyuan Zhang, Zhouyu Wang, Shan Qian
Published 2020-01-01

Design, synthesis and biological evaluation of novel 1H-1,2,4-triazole, benzothiazole and indazole-based derivatives as potent FGFR1 inhibitors viafragment-based virtual screening

by Jian Liu, Yu Wen, Lina Gao, Liang Gao, Fengjun He, Jingxian Zhou, Junwei Wang, Rupeng Dai, Xiaojing Chen, Di Kang, Lihong Hu
Published 2020-01-01

Recent advances in modulators of circadian rhythms: an update and perspective

by Shenzhen Huang, Xinwei Jiao, Dingli Lu, Xiaoting Pei, Di Qi, Zhijie Li
Published 2020-01-01

6,7-Dimethoxy-2-phenethyl-1,2,3,4-tetrahydroisoquinoline amides and corresponding ester isosteres as multidrug resistance reversers

by Laura Braconi, Gianluca Bartolucci, Marialessandra Contino, Niccolò Chiaramonte, Roberta Giampietro, Dina Manetti, Maria Grazia Perrone, Maria Novella Romanelli, Nicola Antonio Colabufo, Chiara Riganti, Silvia Dei, Elisabetta Teodori
Published 2020-01-01

Topoisomerases inhibition and DNA binding mode of daunomycin–oligoarginine conjugate

by Valeria Visone, Ildikó Szabó, Giuseppe Perugino, Ferenc Hudecz, Zoltán Bánóczi, Anna Valenti
Published 2020-01-01

Activation studies of the β-carbonic anhydrases from Escherichia coli with amino acids and amines

by Alessio Nocentini, Sonia Del Prete, Margaret D. Mastrolorenzo, William A. Donald, Clemente Capasso, Claudiu T. Supuran
Published 2020-01-01

Synthesis and evaluation of AKR1C inhibitory properties of A-ring halogenated oestrone derivatives

by Maša Sinreih, Rebeka Jójárt, Zoltán Kele, Tomaž Büdefeld, Gábor Paragi, Erzsébet Mernyák, Tea Lanišnik Rižner
Published 2021-01-01