scholarly journals useful-anti-cancer-agents-of-natural-product-origin/#

2017 ◽  
Vol 2 (7) ◽  
Keyword(s):  
Natural Product ◽  
Anti Cancer ◽  
Product Origin

Stereoselective Synthesis of Pyroglutamate Natural Product Analogs from α- Aminoacids and their Anti-Cancer Evaluation

2013 ◽  
Vol 13 (10) ◽  
pp. 1514-1530 ◽  
Author(s):  
Srinivas Tekkam ◽  
Mohammad Alam ◽  
Matthew Just ◽  
Steven Berry ◽  
Joseph Johnson ◽  
...  
Keyword(s):  
Natural Product ◽  
Stereoselective Synthesis ◽  
Anti Cancer

scholarly journals Corrigendum to “Natural product inspired allicin analogs as novel anti-cancer agents” [Bioorg. Chem. 86 (2019) 259–272]

2021 ◽  
Vol 110 ◽  
pp. 104780
Author(s):  
Ishani Bhaumik ◽  
Kunal Pal ◽  
Utsab Debnath ◽  
Parimal Karmakar ◽  
Kuladip Jana ◽  
...  
Keyword(s):  
Natural Product ◽  
Anti Cancer

scholarly journals Total Syntheses of Pladienolide-Derived Spliceosome Modulators

Molecules ◽  
2021 ◽  
Vol 26 (19) ◽  
pp. 5938
Author(s):  
Jaehoon Sim ◽  
Eunbin Jang ◽  
Hyun Jin Kim ◽  
Hongjun Jeon
Keyword(s):  
Total Synthesis ◽  
Natural Product ◽  
Structural Features ◽  
Synthetic Approach ◽  
Synthetic Analog ◽  
Phase I Clinical Trials ◽  
Total Syntheses ◽  
Naturally Occurring ◽  
Anti Cancer ◽  
Synthetic Approaches

Pladienolides, an emerging class of naturally occurring spliceosome modulators, exhibit interesting structural features, such as highly substituted 12-membered macrocycles and epoxide-containing diene side chains. The potential of pladienolides as anti-cancer agents is confirmed by H3B-8800, a synthetic analog of this natural product class, which is currently under Phase I clinical trials. Since its isolation in 2004 and the first total synthesis in 2007, a dozen total syntheses and synthetic approaches toward the pladienolide class have been reported to date. This review focuses on the eight completed total syntheses of naturally occurring pladienolides or their synthetic analogs, in addition to a synthetic approach to the main framework of the natural product.

scholarly journals Synthesis and Biological Evaluation of Genistein-IR783 Conjugate: Cancer Cell Targeted Delivery in MCF-7 for Superior Anti-Cancer Therapy

Molecules ◽  
2019 ◽  
Vol 24 (22) ◽  
pp. 4120 ◽  
Author(s):  
Yang Guan ◽  
Yi Zhang ◽  
Juan Zou ◽  
Li-Ping Huang ◽  
Mahendra D. Chordia ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Therapy ◽  
Natural Product ◽  
Cancer Cell ◽  
Biological Evaluation ◽  
Cyanine Dye ◽  
Therapeutic Window ◽  
Anti Cancer ◽  
Mcf 7

The flavonoid-based natural product genistein is a biologically active compound possessing promising anti-oxidant and anti-cancer properties. Poor pharmacokinetics along with low potency limit however the therapeutic application of genistein in cancer therapy. In order to overcome those limitations and to expand its therapeutic window of efficacy, we sought to covalently attach genistein with a heptamethine cyanine dye—IR 783—for cancer cell targeting and enhanced delivery to tumors. Herein we report the synthesis, a selective detailed characterization and preliminary in vitro/in vivo biological evaluation of genistein-IR 783 conjugate 4. The conjugate 4 displayed improved potency against human breast cancer MCF-7 cells (10.4 ± 1.0 μM) as compared with the parent genistein (24.8 ± 0.5 μM) or IR 783 (25.7 ± 0.7 μM) and exhibited selective high uptake in MCF-7 as against the normal mammary gland MCF-10A cells in various assays. In the cell viability assay, conjugate 4 exhibited over threefold lower potency against MCF-10A cells (32.1 ± 1.1 μM) suggesting that the anti-cancer profile of parent genistein is significantly improved upon conjugation with the dye IR783. Furthermore, the genistein-IR783 conjugate 4 was shown to be especially accumulated in MCF-7 cancer cells by fluorescent intensity measurements and inverted fluorescence microscopy in fixed cells as well as in live cells with time via live cell confocal fluorescence imaging. The mechanism-based uptake inhibition of conjugate 4 was observed with OATPs inhibitor BSP and in part with amiloride, as a macropinocytosis inhibitor. For the first time we have shown amiloride inhibited uptake of cyanine dye by about ~40%. Finally, genistein-IR 783 conjugate 4 was shown to be localized in MCF-7 tumor xenografts of mice breast cancer model via in vivo near infrared fluorescence (NIRF) imaging. In conclusion, conjugation of genistein with cyanine dye IR783 indeed improved its pharmacological profile by cancer cell selective uptake and targeting and therefore warrants further investigations as a new anti-cancer therapeutics derived from natural product genistein.

scholarly journals Defining desirable natural product derived anticancer drug space: optimization of molecular physicochemical properties and ADMET attributes

ADMET & DMPK ◽  
2016 ◽  
Vol 4 (2) ◽  
pp. 98 ◽  
Author(s):  
Deepika Singh
Keyword(s):  
Hydrogen Bond ◽  
Natural Products ◽  
Physicochemical Properties ◽  
Natural Product ◽  
Aqueous Solubility ◽  
Cancer Drug ◽  
Log P ◽  
Drug Candidates ◽  
Anti Cancer ◽  
Property Space

<p class="ADMETabstracttext">As part of our endeavor to enhance survival of natural product derived drug candidates and to guide the medicinal chemist to design higher probability space for success in the anti cancer drug development area, we embarked on a detailed study of the property space for a collection of natural product derived anti cancer molecules. We carried out a comprehensive analysis of properties for 24 natural products derived anti cancer drugs including clinical development candidates and a set of 27 natural products derived anti cancer lead compounds. In particular, we focused on understanding the interplay among eight physicochemical properties including like partition coefficient (log P), distribution coefficient at pH=7.4 (log D), topological polar surface area (TPSA), molecular weight (MW), aqueous solubility (log S), number of hydrogen bond acceptors (HBA), number of hydrogen bond donors (HBD) and number of rotatable bonds (n<sub>Rot</sub>) crucial for drug design and  relationships between physicochemical properties, ADME (absorption, distribution, metabolism, and elimination) attributes, and in silico toxicity profile for these two sets of compounds. This analysis provides guidance for the chemist to modify the existing natural product scaffold or designing of new anti cancer molecules in a property space with increased probability of success and may lead to the identification of druglike candidates with favorable safety profiles that can successfully test hypotheses in the clinic.</p>

Large-Scale Synthesis of the anti-Cancer Marine Natural Product (+)-Discodermolide. Part 1. Synthetic Strategy and Preparation of a Common Precursor (I).

ChemInform ◽  
2004 ◽  
Vol 35 (24) ◽  
Author(s):  
Stuart J. Mickel ◽  
Gottfried H. Sedelmeier ◽  
Daniel Niederer ◽  
Robert Daeffler ◽  
Adnan Osmani ◽  
...  
Keyword(s):  
Natural Product ◽  
Large Scale ◽  
Marine Natural Product ◽  
Synthetic Strategy ◽  
Common Precursor ◽  
Anti Cancer ◽  
Large Scale Synthesis

Large-Scale Synthesis of the Anti-Cancer Marine Natural Product (+)-Discodermolide. Part 1:  Synthetic Strategy and Preparation of a Common Precursor

2004 ◽  
Vol 8 (1) ◽  
pp. 92-100 ◽  
Author(s):  
Stuart J. Mickel ◽  
Gottfried H. Sedelmeier ◽  
Daniel Niederer ◽  
Robert Daeffler ◽  
Adnan Osmani ◽  
...  
Keyword(s):  
Natural Product ◽  
Large Scale ◽  
Marine Natural Product ◽  
Synthetic Strategy ◽  
Common Precursor ◽  
Anti Cancer ◽  
Large Scale Synthesis

Redox modulatory and Anti-cancer property of Toluquinol, a marine fungus derived natural product

2017 ◽  
Vol 112 ◽  
pp. 27
Author(s):  
Ankit Khandelwal ◽  
Himadri Bhatt ◽  
Tejal Gajaria ◽  
Vihas T Vasu
Keyword(s):  
Natural Product ◽  
Marine Fungus ◽  
Anti Cancer

scholarly journals Natural product extracts of the Canadian prairie plant,Thermopsis rhombifolia,have anti-cancer activity in phenotypic cell-based assays

2014 ◽  
Vol 29 (11) ◽  
pp. 1026-1034 ◽  
Author(s):  
Sophie Kernéis ◽  
Lucy H. Swift ◽  
Cody W. Lewis ◽  
Céline Bruyère ◽  
Nassima Oumata ◽  
...  
Keyword(s):  
Natural Product ◽  
Canadian Prairie ◽  
Anti Cancer ◽  
Prairie Plant ◽  
Cancer Activity
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