Results 21 to 30 of about 132,855 (268)

Structure-based design of novel heterocycle-substituted ATDP analogs as non-nucleoside reverse transcriptase inhibitors with improved selectivity and solubility

Acta Pharmaceutica Sinica B, 2023
Following on our recently developed biphenyl-ATDP non-nucleoside reverse transcriptase inhibitor ZLM-66 (SI = 2019.80, S = 1.9 μg/mL), a series of novel heterocycle-substituted ATDP derivatives with significantly improved selectivity and solubility were ...
Li-Min Zhao, Christophe Pannecouque, Erik De Clercq, Shuai Wang, Fen-Er Chen   +4 more
doaj   +1 more source

Improving the positional adaptability: structure-based design of biphenyl-substituted diaryltriazines as novel non-nucleoside HIV-1 reverse transcriptase inhibitors

Acta Pharmaceutica Sinica B, 2020
In order to improve the positional adaptability of our previously reported naphthyl diaryltriazines (NP-DATAs), synthesis of a series of novel biphenyl-substituted diaryltriazines (BP-DATAs) with a flexible side chain attached at the C-6 position is ...
Kaijun Jin, Minjie Liu, Chunlin Zhuang, Erik De Clercq, Christophe Pannecouque, Ge Meng, Fener Chen   +6 more
doaj   +1 more source

Chiral Syn-1,3-diol Derivatives via a One-Pot Diastereoselective Carboxylation/ Bromocyclization of Homoallylic Alcohols

iScience, 2018
Summary: Chiral syn-1,3-diols are fundamental structural motifs in many natural products and drugs. The traditional Narasaka-Prasad diastereoselective reduction from chiral β-hydroxyketones is an important process for the synthesis of these ...
Guanxin Huang, Minjie Liu, Fangjun Xiong, Ge Meng, Yuan Tao, Yan Wu, Haihui Peng, Fener Chen   +7 more
doaj   +1 more source

Synthesis and Applications of Asymmetric Catalysis Using Chiral Ligands Containing Quinoline Motifs

SynOpen, 2022
In the past decade, asymmetric synthesis of chiral ligands containing quinoline motifs, a family of natural products displaying a broad range of structural diversity and their metal complexes, have become the most significant methodology for the ...
Vasudevan Dhayalan, Rambabu Dandela, K. Bavya Devi, Ragupathy Dhanusuraman   +3 more
doaj   +1 more source

Chemical asymmetric synthesis

Nature, 1989
Thalidomide comes in two forms: a left-handed compound which is a powerful tranquilizer, and a right-handed version which can disrupt fetal development causing severe handicap. As a necessary consequence of synthetic methods available in the early 1960s the two forms were present in equal proportions in the manufactured drug, with catastrophic ...
Brown, J, Davies, S
openaire   +2 more sources

Computational and Experimental Studies on the α-Functionalization of Ketones Using Domino Reactions: A Strategy to Increase Chemoselectivity at the α-Carbon of Ketones

Molecules
A facile strategy to increase the chemoselectivity of domino reactions was proposed and successfully applied in the α-functionalization of ketones.
Hui Sun, Li-Heng Yang, Meng-Yun Fu, Bin Cui   +3 more
doaj   +1 more source

MCM-41-supported L-phenylalaninol as a chiral heterogeneous ligand in the enantioselective Kharasch-Sosnovsky reaction

Results in Chemistry
In this study, L-phenylalaninol, synthesized from the reduction of naturally occurring L-phenylalanine, was immobilized on MCM-41. The resulting heterogeneous ligand was comprehensively characterized using various spectroscopic techniques, such as FT-IR,
Saadi Samadi, Shadi Kamangar, Hamid Arvinnezhad, Parya Noori   +3 more
doaj   +1 more source

Therapeutic Effects of Coumarins with Different Substitution Patterns

Molecules, 2023
The use of derivatives of natural and synthetic origin has gained attention because of their therapeutic effects against human diseases. Coumarins are one of the most common organic molecules and are used in medicine for their pharmacological and ...
Virginia Flores-Morales, Ana P. Villasana-Ruíz, Idalia Garza-Veloz, Samantha González-Delgado, Margarita L. Martinez-Fierro   +4 more
doaj   +1 more source

Asymmetric Total Synthesis of Pseurotin A [PDF]

Organic Letters, 2003
The asymmetric total syntheses of pseurotin A and 8-O-demethylpseurotin A have been accomplished. Key reactions are a NaH-promoted intramolecular cyclization of an alkynylamide to form a gamma-lactam, an aldol reaction of a benzylidene-substituted ketone, and the late-stage introduction of the benzoyl group by a selective oxidation of a benzylidene ...
Yujiro, Hayashi, Mitsuru, Shoji, Shinpei, Yamaguchi, Takasuke, Mukaiyama, Junichiro, Yamaguchi, Hideaki, Kakeya, Hiroyuki, Osada   +6 more
openaire   +2 more sources

Anticancer Activities of Novel Nicotinamide Phosphoribosyltransferase Inhibitors in Hematological Malignancies

Molecules, 2023
Targeting cancer cells that are highly dependent on the nicotinamide adenine dinucleotide (NAD+) metabolite is a promising therapeutic strategy. Nicotinamide phosphoribosyltransferase (NAMPT) is the rate-limiting enzyme catalyzing NAD+ production ...
Paulina Biniecka, Saki Matsumoto, Axel Belotti, Jessie Joussot, Jian Fei Bai, Somi Reddy Majjigapu, Paul Thoueille, Dany Spaggiari, Vincent Desfontaine, Francesco Piacente, Santina Bruzzone, Michele Cea, Laurent A. Decosterd, Pierre Vogel, Alessio Nencioni, Michel A. Duchosal, Aimable Nahimana   +16 more
doaj   +1 more source