Bioorganic and Medicinal Chemistry Letters This is an RSS file. You can use it to subscribe to this data in your favourite RSS reader or to display this data on your own website or blog.

Synthesis and antiproliferative activity of a tetrahydrofuran analog of FR901464
This study shows the significance of the tetrahydropyran ring that presents the epoxide toward the spliceosome.PMID:38599298 | DOI:10.1016/j.bmcl.2024.129739 (Source: Bioorganic and Medicinal Chemistry Letters)
Source: Bioorganic and Medicinal Chemistry Letters - April 10, 2024 Category: Chemistry Authors: Ivanna Pohorilets Jacob P Beard Julia L Driscoll John C Schmitz Kazunori Koide Source Type: research

The mechanism of covalent inhibition of LAR phosphatase by illudalic acid
Bioorg Med Chem Lett. 2024 Apr 8:129740. doi: 10.1016/j.bmcl.2024.129740. Online ahead of print.ABSTRACTLeukocyte antigen-related (LAR) phosphatase is a receptor-type protein tyrosine phosphatase involved in cellular signaling and associated with human disease including cancer and metabolic disorders. Selective inhibition of LAR phosphatase activity by well characterized and well validated small molecules would provide key insights into the roles of LAR phosphatase in health and disease, but identifying selective inhibitors of LAR phosphatase activity has been challenging. Recently, we described potent and selective inhibi...
Source: Bioorganic and Medicinal Chemistry Letters - April 10, 2024 Category: Chemistry Authors: Daniel T Hansen Nicole J Rueb Nathan D Levinzon Thomas E Cheatham Robert Gaston Kh Tanvir Ahmed Sandra Osburn-Staker James E Cox Gregory B Dudley Amy M Barrios Source Type: research

Structural modification of tanshinone IIA and their α-glucosidase inhibitory activity
Bioorg Med Chem Lett. 2024 Apr 8:129736. doi: 10.1016/j.bmcl.2024.129736. Online ahead of print.ABSTRACTα-Glucosidase is one of the therapeutic approaches for treating type 2 diabetes mellitus. Almost 95 % of diabetes patients worldwide have been diagnosed with type 2 diabetes, resulting in 1.5 million fatalities each year. Newly synthesized oxazole-based tanshinone IIA derivatives (1a-n) were designed and evaluated for their inhibitory activity against α-glucosidase enzyme. Eight compounds (1a-d, 1f-g, 1j, and 1m) demonstrated excellent inhibition with IC50 values ranging from 0.73 ± 0.11 to 9.46 ± 0.57 μM as compare...
Source: Bioorganic and Medicinal Chemistry Letters - April 10, 2024 Category: Chemistry Authors: Mutita Kongphet Hoa Tai Xuan Hang Thanh The Ngo Thi-Kim-Dung Le Warinthorn Chavasiri Source Type: research

Insights into the structure-activity relationship of the anticancer compound ZJ-101: A role played by the amide moiety
Bioorg Med Chem Lett. 2024 Apr 8:129741. doi: 10.1016/j.bmcl.2024.129741. Online ahead of print.ABSTRACTZJ-101, a structurally simplified analog of marine natural product superstolide A, was previously designed and synthesized in our laboratory. In the present study four new analogs of ZJ-101 were designed and synthesized to investigate the structure-activity relationship of the acetamide moiety of the molecule. The biological evaluation showed that the amide moiety is important for the molecule's anticancer activity. Replacing the amide with other unctional groups such as a sulfonamide group, a carbamate group, and a urea...
Source: Bioorganic and Medicinal Chemistry Letters - April 10, 2024 Category: Chemistry Authors: Haibo Qiu Shan Qian Sarah A Head Phillip R Sanchez Jun O Liu Zhendong Jin Source Type: research

The discovery of an anti-inflammatory monoterpenoid, neoroseoside from the Zea mays
Bioorg Med Chem Lett. 2024 Apr 8:129737. doi: 10.1016/j.bmcl.2024.129737. Online ahead of print.ABSTRACTA new monoterpenoid, neoroseoside (1), along with two previously reported compounds, 2″-O-α-l-rhamnosyl-6-C-fucosylluteolin (2) and farobin A (3) were isolated from the Zea mays. The structure of compound 1 was determined through the analysis spectroscopic data, including mass spectrometry (MS), infrared (IR) spectroscopy, and nuclear magnetic resonance (NMR) data. The absolute configurations of 1 were deduced from the comparing the values of optical rotations and from the interpretation of electronic circular dichroi...
Source: Bioorganic and Medicinal Chemistry Letters - April 10, 2024 Category: Chemistry Authors: Hui Tan Hyun-Jin Lee Prima F Hillman Eun-Young Lee Chaeyoung Lee Eun Kyoung Seo Mi Ja Lee Sang-Jip Nam Source Type: research

Copper-mediated siRNA activation for conditional control of gene expression
We present a chemical approach of selective siRNA activation triggered by intracellular copper ions. We designed and synthesized nucleotides containing copper-responsive moieties, which were incorporated into siRNAs. These copper-responsive siRNAs effectively silenced the target cyclin B1 mRNA in living cells. This pioneering study introduces a novel method for conditionally controlling gene silencing using biologically relevant metal ions in human cells, thereby expanding the repertoire of chemical knockdown tools.PMID:38593925 | DOI:10.1016/j.bmcl.2024.129738 (Source: Bioorganic and Medicinal Chemistry Letters)
Source: Bioorganic and Medicinal Chemistry Letters - April 9, 2024 Category: Chemistry Authors: Kunihiko Morihiro Yasuhiro Tomida Honami Ando Akimitsu Okamoto Source Type: research

Discovery of N-(1,4-Benzoxazin-3-one) urea analogs as Mode-Selective TRPV1 antagonists
Bioorg Med Chem Lett. 2024 Apr 6:129735. doi: 10.1016/j.bmcl.2024.129735. Online ahead of print.ABSTRACTA series of 1,4-benzoxazin-3-one analogs were investigated to discover mode-selective TRPV1 antagonists, since such antagonists are predicted to minimize target-based adverse effects. Using the high-affinity antagonist 2 as the lead structure, the structure activity relationship was studied by modifying the A-region through incorporation of a polar side chain on the benzoxazine and then by changing the C-region with a variety of substituted pyridine, pyrazole and thiazole moieties. The t-butyl pyrazole and thiazole C-reg...
Source: Bioorganic and Medicinal Chemistry Letters - April 8, 2024 Category: Chemistry Authors: Guocheng Huang Aeran Jung Li-Xuan Li Nayeon Do Sungwon Jung Yubum Jeon Dongxu Zuo Minh Thanh La Nguyen Van Manh Peter M Blumberg Hongryul Yoon Yoonji Lee Jihyae Ann Jeewoo Lee Source Type: research

[ < sup > 99m < /sup > Tc]Tc-labeled HYNIC conjugated chlorambucil as a tumor targeting Agent: Synthesis, characterization and ex-vivo evaluation
Bioorg Med Chem Lett. 2024 Apr 5:129730. doi: 10.1016/j.bmcl.2024.129730. Online ahead of print.ABSTRACTChlorambucil is an alkylating drug that finds application towards chemotherapy of different types of cancers. In order to explore the possibility of utilization of this drug as an imaging agent for early diagnosis of solid tumors, attempt was made to synthesize a 99mTc complex of chlorambucil and evaluate its potential in tumor bearing small animal model. HYNIC-chlorambucil (HYNIC is hydrazine nicotinamide) was synthesized by conjugation of HYNIC with chlorambucil via an ethylenediamine linker. All the intermediates and ...
Source: Bioorganic and Medicinal Chemistry Letters - April 7, 2024 Category: Chemistry Authors: Soumi Kolay Naveen Kumar Mohini Guleria Tapas Das Source Type: research

Systematical mutational analysis of teriparatide on anti-osteoporosis activity by alanine scanning
Bioorg Med Chem Lett. 2024 Apr 5;104:129732. doi: 10.1016/j.bmcl.2024.129732. Online ahead of print.ABSTRACTOsteoporosis is a progressive systemic skeletal disease that decreases bone density and bone quality, making them fragile and easy to break. In spite of effective anti-osteoporosis potency, teriparatide, the first anabolic medications approved for the treatment of osteoporosis, was proven to exhibit various side effects. And the relevant structure-activity relationship (SAR) of teriparatide was in need. In this work, we performed a systematical alanine scanning against teriparatide and synthesized 34 teriparatide der...
Source: Bioorganic and Medicinal Chemistry Letters - April 7, 2024 Category: Chemistry Authors: Haiyan Liang Huaxing Shen Mengjun Zheng Yejiao Shi Xiang Li Source Type: research

A responsive disulfide bond switch aptamer prodrug exhibiting enhanced stability and anticancer efficacy
Bioorg Med Chem Lett. 2024 Apr 5:129729. doi: 10.1016/j.bmcl.2024.129729. Online ahead of print.ABSTRACTAptamers have shown significant potential in treating diverse diseases. However, challenges such as stability and drug delivery limited their clinical application. In this paper, the development of AS1411 prodrug-type aptamers for tumor treatment was introduced. A Short oligonucleotide was introduced at the end of the AS1411 sequence with a disulfide bond as responsive switch. The results indicated that the aptamer prodrugs not only enhanced the stability of the aptamer against nuclease activity but also facilitated bind...
Source: Bioorganic and Medicinal Chemistry Letters - April 7, 2024 Category: Chemistry Authors: Xiao Dong Zhe Zhang Tangna Zhao Zuyi Chen Jia Wang Liang Xu Aiping Zhang Source Type: research

Systematical mutational analysis of teriparatide on anti-osteoporosis activity by alanine scanning
Bioorg Med Chem Lett. 2024 Apr 5:129732. doi: 10.1016/j.bmcl.2024.129732. Online ahead of print.ABSTRACTOsteoporosis is a progressive systemic skeletal disease that decreases bone density and bone quality, making them fragile and easy to break. In spite of effective anti-osteoporosis potency, teriparatide, the first anabolic medications approved for the treatment of osteoporosis, was proven to exhibit various side effects. And the relevant structure-activity relationship (SAR) of teriparatide was in need. In this work, we performed a systematical alanine scanning against teriparatide and synthesized 34 teriparatide derivat...
Source: Bioorganic and Medicinal Chemistry Letters - April 7, 2024 Category: Chemistry Authors: Haiyan Liang Huaxing Shen Mengjun Zheng Yejiao Shi Xiang Li Source Type: research