A series of 49 oxygenated tricyclic carbazole derivatives has been tested for inhibition of the growth of Mycobacterium tuberculosis and a mammalian cell line (vero cells). From this series, twelve carbazoles showed a significant anti-TB activity. The four most active compounds were the naturally occurring carbazole alkaloids clauszoline-M (45), murrayaline-C (41), carbalexin-C (27), and the synthetic carbazole derivative 22 with MIC values ranging from 1.5 to 3.7μM. The active compounds were virtually nontoxic for the mammalian cell line in the concentration range up to 50μM.
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http://dx.doi.org/10.1016/j.bmc.2016.12.038 | DOI Listing |
Mar Drugs
November 2024
BB21 Plus Program, Department of Chemistry, Pukyong National University, Busan 48513, Republic of Korea.
Melanoma is an aggressive skin cancer with a high risk of cancer-related deaths, and inducing apoptosis in melanoma cells is a promising therapeutic strategy. This study investigates the anti-tumor potential of a novel lucknolide derivative LA-UC as a therapeutic candidate for melanoma. Lucknolide A (LA), a tricyclic ketal-lactone metabolite isolated from marine-derived sp.
View Article and Find Full Text PDFOrg Lett
November 2024
Laboratory of Medicinal Chemistry, Chulabhorn Research Institute, 54 Kamphaeng Phet 6 Laksi, Bangkok, 10210, Thailand.
An unprecedented Bi(OTf)-catalyzed reaction between 2-arylisatogens and vinylarenes to yield 2,4-diarylquinolines is reported. The transformation occurred via a Bi-coordination to the embedded anionic nitrone oxygen, which induced a regiospecific stepwise formal [4 + 2]-cycloaddition with vinylarenes to yield a strained tricyclic intermediate, which subsequently extruded gaseous carbon monoxide. -Deoxygenative aromatization ensued to produce 2,4-diarylquinolines.
View Article and Find Full Text PDFJ Nat Prod
October 2024
School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, Wuhan 430030, People's Republic of China.
ACS Omega
September 2024
Geology and Geophysics Department, College of Science, King Saud University, 11362 Riyadh, Saudi Arabia.
The Early Cretaceous clay-rich facies of the Sembar Formation represent the most significantly occurring organic-rich sediments in the Southern Indus Basin of Pakistan. In this study, detailed geochemical research of total organic carbon, biomarker, mineralogy and trace elemental compositions, together with kerogen microscopic analysis, were carried out and used to understand the organic matter input and the dispositional environmental setting of the organic-rich Sembar shale. The Sembar shales have high organic matter, as indicated by the total organic carbon (TOC) content of up to 2.
View Article and Find Full Text PDFNaunyn Schmiedebergs Arch Pharmacol
September 2024
Department of General and Pediatric Surgery, Faculty of Medicine, Tanta University, Second Tanta, Gharbia Governorate, Egypt.
Diisononyl phthalate (DiNP) has been associated with the development of allergies, asthma, and allergic airway inflammation. Through a complex interplay of signals and feedback mechanisms, the lungs communicate with the heart to ensure maintenance of homeostasis and supporting the body's metabolic demands. In the current study, we assessed the crosstalk between DiNP-induced asthma and cardiac cellular respiration, oxidative stress, apoptotic potential, and induction of oncogenic factors.
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