Publication Title ("European Journal of Medicinal Chemistry") And Id (5MVQ) And Date (Nov 15, 2022) And Volume Number (242) - Results

Select Design, synthesis, and biological evaluation of novel dual inhibitors of heat shock protein 90/mammalian target of rapamycin (Hsp90/mTOR) against bladder cancer cells.

1

Design, synthesis, and biological evaluation of novel dual inhibitors of heat shock protein 90/mammalian target of rapamycin (Hsp90/mTOR) against bladder cancer cells.

Authors:Zhaoping Pan, Yi Chen, Haiying Pang, Xiaoyun Wang, Yuehua Zhang, Xin Xie, et al.From:European Journal of Medicinal Chemistry (Vol. 242) Peer-Reviewed

Nov. 15, 2022372 words Report, Brief articl...

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Select Discovery of azaspirocyclic 1H-3,4,5-Trisubstitued pyrazoles as novel G2019S-LRRK2 selective kinase inhibitors.

2

Discovery of azaspirocyclic 1H-3,4,5-Trisubstitued pyrazoles as novel G2019S-LRRK2 selective kinase inhibitors.

Authors:Robert K. Lesniak, R. Jeremy Nichols, Marcus Schonemann, Jing Zhao, Chandresh R. Gajera, Grace Lam, et al.From:European Journal of Medicinal Chemistry (Vol. 242) Peer-Reviewed

Nov. 15, 2022341 words Report, Brief articl...

Abstract Only

Select Discovery of novel PDE4 inhibitors targeting the M-pocket from natural mangostanin with improved safety for the treatment of Inflammatory Bowel Diseases.

3

Discovery of novel PDE4 inhibitors targeting the M-pocket from natural mangostanin with improved safety for the treatment of Inflammatory Bowel Diseases.

Authors:Haobai Liu, Quan Wang, Yue Huang, Jinhui Deng, Xi Xie, Jiaqi Zhu, et al.From:European Journal of Medicinal Chemistry (Vol. 242) Peer-Reviewed

Nov. 15, 2022379 words Report, Brief articl...

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Select Design, synthesis and biological evaluation of (Quinazoline 4-yloxy)acetamide and (4-oxoquinazoline-3(4H)-yl)acetamide derivatives as inhibitors of Mycobacterium tuberculosis bd oxidase.

4

Design, synthesis and biological evaluation of (Quinazoline 4-yloxy)acetamide and (4-oxoquinazoline-3(4H)-yl)acetamide derivatives as inhibitors of Mycobacterium tuberculosis bd oxidase.

Authors:Amit Kumar, Neetu Kumari, Sandeep Bhattacherjee, Umamageswaran Venugopal, Shahid Parwez, Mohammad Imran Siddiqi, et al.From:European Journal of Medicinal Chemistry (Vol. 242) Peer-Reviewed

Nov. 15, 2022384 words Report, Brief articl...

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Select Synthesis and evaluation of novel furanones as biofilm inhibitors in opportunistic human pathogens.

5

Synthesis and evaluation of novel furanones as biofilm inhibitors in opportunistic human pathogens.

Authors:Andromeda-Celeste Gómez, Thérèse Lyons, Uwe Mamat, Daniel Yero, Marc Bravo, Xavier Daura, et al.From:European Journal of Medicinal Chemistry (Vol. 242) Peer-Reviewed

Nov. 15, 2022410 words Report

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Select Discovery of substituted benzyloxy-benzylamine inhibitors of acetyltransferase Eis and their anti-mycobacterial activity.

6

Discovery of substituted benzyloxy-benzylamine inhibitors of acetyltransferase Eis and their anti-mycobacterial activity.

Authors:Allan H. Pang, Keith D. Green, Nishad Thamban Chandrika, Atefeh Garzan, Ankita Punetha, Selina Y.L. Holbrook, et al.From:European Journal of Medicinal Chemistry (Vol. 242) Peer-Reviewed

Nov. 15, 2022340 words Report, Brief articl...

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Select Discovery of novel benzbromarone analogs with improved pharmacokinetics and benign toxicity profiles as antihyperuricemic agents.

7

Discovery of novel benzbromarone analogs with improved pharmacokinetics and benign toxicity profiles as antihyperuricemic agents.

Authors:Zean Zhao, Jin Liu, Lin Yuan, Zichao Yang, Peihua Kuang, Hui Liao, et al.From:European Journal of Medicinal Chemistry (Vol. 242) Peer-Reviewed

Nov. 15, 2022448 words Report

Abstract Only

Select Development of fluorizoline analogues as prohibitin ligands that modulate C-RAF signaling, p21 expression and melanogenesis.

8

Development of fluorizoline analogues as prohibitin ligands that modulate C-RAF signaling, p21 expression and melanogenesis.

Authors:Nora Chouha, Hussein Abou-Hamdan, Hajime Yurugi, Riku Yoshii, Hiromi Ii, Ahmad Najem, et al.From:European Journal of Medicinal Chemistry (Vol. 242) Peer-Reviewed

Nov. 15, 2022388 words Report, Brief articl...

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Select The discovery of novel antifungal phenylpyridines derivatives based on CYP53 binding model.

9

The discovery of novel antifungal phenylpyridines derivatives based on CYP53 binding model.

Authors:Bin Sun, Yating Liu, Haiyan Fan, Yunfei An, Wenxia Liu, Qingpeng Wang, et al.From:European Journal of Medicinal Chemistry (Vol. 242) Peer-Reviewed

Nov. 15, 2022299 words Report, Brief articl...

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Select (1R,3S)-THCCA-Asn: To show the discovery of selective inhibitor of thrombin by successfully combining virtual screening and biological assay.

10

(1R,3S)-THCCA-Asn: To show the discovery of selective inhibitor of thrombin by successfully combining virtual screening and biological assay.

Authors:Xiaoyi Zhang, Yifan Yang, Yuji Wang, Jianhui Wu, Qiongyan Fang, Yaonan Wang, et al.From:European Journal of Medicinal Chemistry (Vol. 242) Peer-Reviewed

Nov. 15, 2022413 words Report

Abstract Only

Select Development and structure-activity relationship of tacrine derivatives as highly potent CDK2/9 inhibitors for the treatment of cancer.

11

Development and structure-activity relationship of tacrine derivatives as highly potent CDK2/9 inhibitors for the treatment of cancer.

Authors:Limeng Wu, Wenjie Liu, Yaoguang Huang, Chengze Zhu, Qun Ma, Qiong Wu, et al.From:European Journal of Medicinal Chemistry (Vol. 242) Peer-Reviewed

Nov. 15, 2022440 words Report

Abstract Only

Select Synthesis and biological evaluation of novel FiVe1 derivatives as potent and selective agents for the treatment of mesenchymal cancers.

12

Synthesis and biological evaluation of novel FiVe1 derivatives as potent and selective agents for the treatment of mesenchymal cancers.

Authors:Francisco Martínez-Peña, Aaron D. Pearson, Eileen L. Tang, Nick A. Kuburich, Sendurai A. Mani, Peter G. Schultz, et al.From:European Journal of Medicinal Chemistry (Vol. 242) Peer-Reviewed

Nov. 15, 2022445 words Report

Abstract Only

Select Recent advances in [beta]-lactamase inhibitor chemotypes and inhibition modes.

13

Recent advances in [beta]-lactamase inhibitor chemotypes and inhibition modes.

Authors:Rong Li, Xi Chen, Cong Zhou, Qing-Qing Dai, and Lingling YangFrom:European Journal of Medicinal Chemistry (Vol. 242) Peer-Reviewed

Nov. 15, 2022267 words Report, Brief articl...

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Select Site-specific N-terminal PEGylation-based controlled release of biotherapeutics: An application for GLP-1 delivery to improve pharmacokinetics and prolong hypoglycemic effects.

14

Site-specific N-terminal PEGylation-based controlled release of biotherapeutics: An application for GLP-1 delivery to improve pharmacokinetics and prolong hypoglycemic effects.

Authors:Qianmeng Lin, Xuan Xia, Jun Li, Zhan Zhou, and Yongheng ChenFrom:European Journal of Medicinal Chemistry (Vol. 242) Peer-Reviewed

Nov. 15, 2022308 words Report, Brief articl...

Abstract Only

Select Amlexanox-modified platinum(IV) complex triggers apoptotic and autophagic bimodal death of cancer cells.

15

Amlexanox-modified platinum(IV) complex triggers apoptotic and autophagic bimodal death of cancer cells.

Authors:Yan Guo, Suxing Jin, Dongfan Song, Tao Yang, Jiyong Hu, Xiaowei Hu, et al.From:European Journal of Medicinal Chemistry (Vol. 242) Peer-Reviewed

Nov. 15, 2022365 words Brief article

Abstract Only

Select A water-dependent reversible photoacidity strategy for cancer treatment.

16

A water-dependent reversible photoacidity strategy for cancer treatment.

Authors:Lin Kang, Hongyou Zhao, Shiyang Liu, Yupeng Liu, Yidi Liu, Defu Chen, et al.From:European Journal of Medicinal Chemistry (Vol. 242) Peer-Reviewed

Nov. 15, 2022398 words Report, Brief articl...

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Select Current status and progress in using radiolabelled PARP-1 inhibitors for imaging PARP-1 expression in tumours.

17

Current status and progress in using radiolabelled PARP-1 inhibitors for imaging PARP-1 expression in tumours.

Authors:Qianna Wang and Junbo ZhangFrom:European Journal of Medicinal Chemistry (Vol. 242) Peer-Reviewed

Nov. 15, 2022192 words Report, Brief articl...

Abstract Only

Select Development of 3[alpha],7[alpha]-dihydroxy-6[alpha]-ethyl-24-nor-5[beta]-cholan-23-sulfate sodium salt (INT-767): Process optimization, synthesis and characterization of metabolites.

18

Development of 3[alpha],7[alpha]-dihydroxy-6[alpha]-ethyl-24-nor-5[beta]-cholan-23-sulfate sodium salt (INT-767): Process optimization, synthesis and characterization of metabolites.

Authors:Bruno Cerra, Francesco Venturoni, Maria Souma, Giada Ceccarelli, Anna Maria Lozza, Daniela Passeri, et al.From:European Journal of Medicinal Chemistry (Vol. 242) Peer-Reviewed

Nov. 15, 2022356 words Report, Brief articl...

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Select Discovery and evaluation of phenacrylanilide derivatives as novel potential anti-liver fibrosis agents.

19

Discovery and evaluation of phenacrylanilide derivatives as novel potential anti-liver fibrosis agents.

Authors:Lin Yue, Taixiong Xue, Xingping Su, Zhihao Liu, Hongyao Liu, Zui Tan, et al.From:European Journal of Medicinal Chemistry (Vol. 242) Peer-Reviewed

Nov. 15, 2022359 words Report, Brief articl...

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Select New structural classes of antimalarials.

20

New structural classes of antimalarials.

Authors:Gajanan K. Rathod, Meenakshi Jain, Krishna K. Sharma, Samarpita Das, Ahana Basak, and Rahul JainFrom:European Journal of Medicinal Chemistry (Vol. 242) Peer-Reviewed

Nov. 15, 2022296 words Report, Brief articl...

Abstract Only

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Design, synthesis, and biological evaluation of novel dual inhibitors of heat shock protein 90/mammalian target of rapamycin (Hsp90/mTOR) against bladder cancer cells.

Discovery of azaspirocyclic 1H-3,4,5-Trisubstitued pyrazoles as novel G2019S-LRRK2 selective kinase inhibitors.

Discovery of novel PDE4 inhibitors targeting the M-pocket from natural mangostanin with improved safety for the treatment of Inflammatory Bowel Diseases.

Design, synthesis and biological evaluation of (Quinazoline 4-yloxy)acetamide and (4-oxoquinazoline-3(4H)-yl)acetamide derivatives as inhibitors of Mycobacterium tuberculosis bd oxidase.

Synthesis and evaluation of novel furanones as biofilm inhibitors in opportunistic human pathogens.

Discovery of substituted benzyloxy-benzylamine inhibitors of acetyltransferase Eis and their anti-mycobacterial activity.

Discovery of novel benzbromarone analogs with improved pharmacokinetics and benign toxicity profiles as antihyperuricemic agents.

Development of fluorizoline analogues as prohibitin ligands that modulate C-RAF signaling, p21 expression and melanogenesis.

The discovery of novel antifungal phenylpyridines derivatives based on CYP53 binding model.

(1R,3S)-THCCA-Asn: To show the discovery of selective inhibitor of thrombin by successfully combining virtual screening and biological assay.

Development and structure-activity relationship of tacrine derivatives as highly potent CDK2/9 inhibitors for the treatment of cancer.

Synthesis and biological evaluation of novel FiVe1 derivatives as potent and selective agents for the treatment of mesenchymal cancers.

Recent advances in [beta]-lactamase inhibitor chemotypes and inhibition modes.

Site-specific N-terminal PEGylation-based controlled release of biotherapeutics: An application for GLP-1 delivery to improve pharmacokinetics and prolong hypoglycemic effects.

Amlexanox-modified platinum(IV) complex triggers apoptotic and autophagic bimodal death of cancer cells.

A water-dependent reversible photoacidity strategy for cancer treatment.

Current status and progress in using radiolabelled PARP-1 inhibitors for imaging PARP-1 expression in tumours.

Development of 3[alpha],7[alpha]-dihydroxy-6[alpha]-ethyl-24-nor-5[beta]-cholan-23-sulfate sodium salt (INT-767): Process optimization, synthesis and characterization of metabolites.

Discovery and evaluation of phenacrylanilide derivatives as novel potential anti-liver fibrosis agents.

New structural classes of antimalarials.

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