Bioorganic Chemistry
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#1Runlai Liu (SPU: Shenyang Pharmaceutical University)
#2Shuai Zhang (SPU: Shenyang Pharmaceutical University)
Last. Weige Zhang (SPU: Shenyang Pharmaceutical University)H-Index: 7
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Abstract null null Two series of 2,7-diaryl-pyrazolo[1,5-a]pyrimidines as tubulin polymerization inhibitors were designed to restrict bioactive configuration of (E,Z)-vinylogous CA-4. All of the target compounds were synthesized and then evaluated for their in vitro antiproliferative activities against three cancer cell lines (MCF-7, SGC-7901 and A549). Among them, 6d exhibited the most potent antiproliferative activity against the MCF-7 with IC50 value of 0.047 μM. Moreover, 6d significantly in...
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#1Ji-Xue Zou (CAS: Chinese Academy of Sciences)H-Index: 1
#2Yin-Ping Song (CAS: Chinese Academy of Sciences)H-Index: 7
Last. Nai-Yun Ji (CAS: Chinese Academy of Sciences)H-Index: 19
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Abstract null null Ten new bisabolane derivatives, trichobisabolins Q–Z (1–10), one new cadinane derivative, cadin-4-en-11-ol (11), and three new cyclonerane derivatives, cycloner-3-en-7,11-diol (12), isoepicyclonerodiol oxide (13), and norepicyclonerodiol oxide (14), were isolated from the endophytic fungal strain RR-dl-6-11 of Trichoderma asperelloides that was obtained from a marine alga. Their structures along with relative configurations were established mainly by NMR and IR as well as MS t...
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#1Lalitha Gummidi (UKZN: University of KwaZulu-Natal)H-Index: 7
#2Nagaraju Kerru (UKZN: University of KwaZulu-Natal)H-Index: 11
Last. Parvesh Singh (UKZN: University of KwaZulu-Natal)H-Index: 18
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Abstract null null A simple and efficient protocol was developed to synthesize a new library of thiazolidine-4-one molecular hybrids (4a-n) via a one-pot multicomponent reaction involving 5-substituted phenyl-1,3,4-thiadiazol-2-amines, substituted benzaldehydes and 2-mercaptoacetic acid. The synthesized compounds were evaluated in vitro for their antidiabetic activities through α-glucosidase and α-amylase inhibition as well as their antioxidant and antimicrobial potentials. Compound 4e exhibited...
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#1Neda Shakour (MUMS: Mashhad University of Medical Sciences)H-Index: 2
#2Amirhossein Sahebkar (MUMS: Mashhad University of Medical Sciences)H-Index: 104
Last. Farzin Hadizadeh (MUMS: Mashhad University of Medical Sciences)H-Index: 24
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Abstract null null A newly designed series of imidazolyl-methyl- l-2,4-thiazolidinediones 9 (a-m) were synthesized and In Silico studies were carried out to rationalize their anti-diabetic activity. Generally, all newly synthesized thiazolidinediones had anti-hyperglycemic activity compared with a diabetic-control group, without toxicity in 3T3 cells (viability ≥ 90%). These studies revealed that the compounds 9e and 9b ( null null null 11 null ∗ null null null 10 null null null - null 6 null nu...
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#1Ingrid Y. Martínez-Aldino (UNAM: National Autonomous University of Mexico)
#2Martha Villaseca-Murillo (UNAM: National Autonomous University of Mexico)
Last. José Rivera-Chávez (UNAM: National Autonomous University of Mexico)H-Index: 8
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Abstract null null Protein tyrosine phosphatase 1B (PTP1B) is an active target for developing drugs to treat type II diabetes, obesity, and cancer. However, in the past, research programs targeting this enzyme focused on discovering inhibitors of truncated models (hPTP1B1-282, hPTP1B1-298, or hPTP1B1-321), losing valuable information about the ligands' mechanism of inhibition and selectivity. Nevertheless, finding an allosteric site in hPTP1B1-321, and the full-length (hPTP1B1-400) protein expre...
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#1Mayuri S. Prasad (RTMNU: Rashtrasant Tukadoji Maharaj Nagpur University)
#2Ritesh P. BholeH-Index: 7
Last. Rupesh V. Chikhale (UCL: University College London)H-Index: 11
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Abstract null null Enoyl acyl carrier protein reductase (InhA) is a key enzyme involved in fatty acid synthesis mainly mycolic acid biosynthesis that is a part of NADH dependent acyl carrier protein reductase family. The aim of the present literature is to underline the different scaffolds or enzyme inhibitors that inhibit mycolic acid biosynthesis mainly cell wall synthesis by inhibiting enzyme InhA. Various scaffolds were identified based on the screening technologies like high throughput scre...
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#1Yulin Duan (HUST: Huazhong University of Science and Technology)H-Index: 3
#2Yanfang Deng (HUST: Huazhong University of Science and Technology)H-Index: 1
Last. Changxing Qi (HUST: Huazhong University of Science and Technology)H-Index: 11
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Abstract null null Eleven new polycyclic polyprenylated acylphloroglucinols (PPAPs), hyperwilsones A–K (1–11), along with five known PPAPs (12–16), were isolated from Hypericum wilsonii. Their structures were established via spectroscopic methods, the careful analysis of calculated and experimental electronic circular dichroism (ECD) spectra, single-crystal X-ray diffraction, the modified Mosher’s method, and [Rh2(OCOCF3)4]-induced ECD. Hyperwilsone A (1) and hyperwilsone B (2) possessed the uni...
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Abstract null null The comparative study of new proteasome inhibitors based on salicylic acid-modified pseudo-tripeptides terminated with aldehyde or vinylsulfone is presented. We described the synthesis of 11 pairs of pseudopeptides and their properties related to the proteasome inhibition were determined. The effects of integrated amino acids (combinations of leucine, phenylalanine, tryptophan, proline, cyclohexylalanine or norleucine residues) on the activity of the proteasome were investigat...
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#1Sandeepchowdary Bala (Indian Institute of Chemical Technology)
#2Kalisha vali Yellamanda (GITAM: Gandhi Institute of Technology and Management)
Last. Anthony Addlagatta (Indian Institute of Chemical Technology)H-Index: 24
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Abstract null null Methionine aminopeptidases (MetAPs) are an important class of enzymes that work co-translationally for the removal of initiator methionine. Chemical inhibition or gene knockdown is lethal to the microbes suggesting that they can be used as antibiotic targets. However, sequence and structural similarity between the microbial and host MetAPs has been a challenge in the identification of selective inhibitors. In this study, we have analyzed several thousands of MetAP sequences an...
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#1Ahmed Elkamhawy (Mansoura University)H-Index: 10
#2Sora Paik (KIST: Korea Institute of Science and Technology)H-Index: 6
Last. Eun Joo Roh (Kigali Institute of Science and Technology)H-Index: 18
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Abstract null null Up to date, the current clinical practice employs only symptomatic treatments for management of Parkinson's disease (PD) but unable to stop disease progression. The discovery of new chemical entities endowed with potent and selective human monoamine oxidase B (hMAO-B) inhibitory activity is a clinically relevant subject. Herein, a structural optimization strategy for safinamide (a well-known second generation hMAO-B inhibitor) afforded a series of thirty-six safinamide-derived...
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