Synthesis and Evaluation of Novel Compounds with Anticancer Activity

A special issue of Life (ISSN 2075-1729). This special issue belongs to the section "Pharmaceutical Science".

Deadline for manuscript submissions: closed (31 December 2023) | Viewed by 1407

Special Issue Editors


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Guest Editor
Scientific and Educational Center of Pharmaceutics, Kazan (Volga region) Federal University, Kazan, Russia
Interests: chemotherapy; anti-cancer drugs; vitamin B6 (pyridoxine); derivatives of curcumin and dehydrozingerone; preclinical drug study

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Guest Editor
1. Scientific and Educational Center of Pharmaceutics, Kazan (Volga region) Federal University, Kazan, Russia
2. JSC "Tatchempharmpreparaty", Kazan, Russia
Interests: preclinical and clinical drug study; anticancer drugs; analogs of estradiol; ABC transporters; multidrug resistance

Special Issue Information

Dear Colleagues,

Cancer is a leading cause of death worldwide, accounting for nearly 10 million deaths in 2020, or nearly one in six deaths. Drug treatment, together with surgical operation, radiotherapy and biotherapy, constitute the main approaches to cancer treatment. Small molecules—products of chemical synthesis—are still the basis of classical anticancer drugs, such as alkylating agents, antimetabolites, antibiotics, vinca alkaloids, taxanes and topoisomerase inhibitors. Classical anticancer drugs target general biological processes such as DNA synthesis and mitosis and, therefore, are characterized by low selectivity and high cytotoxicity towards rapidly dividing normal cells. Despite this, small molecules still make up 75% of the anticancer drug market, and are cheaper to manufacture, and easier to pack into tablets and capsules for oral use than biological macromolecules. Additionally, small molecules can provide targeted tumor therapy, in particular tyrosine kinase inhibitors, such as imatinib, which block the proliferation of tumor cells that overexpress tyrosine kinases. In this regard, the synthesis and evaluation of small antitumor molecules remains an urgent task for researchers to this day. A newer direction is the synthesis of therapeutic peptides, polypeptides and nucleic acids, which are also of great interest for the development of anticancer drugs. Contributors are encouraged to submit manuscripts and reviews covering but not limited to the following topics:

  • Synthesis of novel analogs of known anticancer agents and evaluation of their biological activity;
  • Synthesis and evaluation of natural alkaloid derivatives (such as curcumin, dehydrozingerone, colchicine, vinca alkaloids and others) with anticancer activity;
  • Synthesis and evaluation of short peptides and polypeptides that can inhibit tumour cell proliferation or migration, or suppress the formation of tumour blood vessels;
  • Development and evaluation of siRNAs, shRNAs and other types of nucleic acids as an effective approach to silence cancer-causing genes.

Dr. Oksana Viktorovna Bondar
Dr. Alfiya Iksanova
Guest Editors

Manuscript Submission Information

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Keywords

  • anticancer agents
  • synthesis
  • design
  • biological activity
  • natural products
  • anticancer peptides
  • anticancer nucleic acids

Published Papers (1 paper)

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Research

27 pages, 5944 KiB  
Article
Anticancer Potential of Pyridoxine-Based Doxorubicin Derivatives: An In Vitro Study
by Rawdah Karwt, Oksana V. Bondar, Mikhail V. Pugachev, Tharaa Mohammad, Aisylu S. Kadyrova, Roman S. Pavelyev, Saleh Alrhmoun, Oleg I. Gnezdilov and Yurii G. Shtyrlin
Life 2024, 14(3), 282; https://doi.org/10.3390/life14030282 - 20 Feb 2024
Viewed by 1139
Abstract
Doxorubicin (DOX) is a prevalent anticancer agent; however, it is unfortunately characterized by high cardiotoxicity, myelosuppression, and multiple other side effects. To overcome DOX limitations, two novel pyridoxine-derived doxorubicin derivatives were synthesized (DOX-1 and DOX-2). In the present study, their antitumor activity and [...] Read more.
Doxorubicin (DOX) is a prevalent anticancer agent; however, it is unfortunately characterized by high cardiotoxicity, myelosuppression, and multiple other side effects. To overcome DOX limitations, two novel pyridoxine-derived doxorubicin derivatives were synthesized (DOX-1 and DOX-2). In the present study, their antitumor activity and mechanism of action were investigated. Of these two compounds, DOX-2, in which the pyridoxine fragment is attached to the doxorubicin molecule via a C3 linker, revealed higher selectivity against specific cancer cell types compared to doxorubicin and a promising safety profile for conditionally normal cells. However, the compound with a C1 linker (DOX-1) was not characterized by selectivity of antitumor action. It was revealed that DOX-2 obstructs cell cycle progression, induces apoptosis via the mitochondrial pathway without the development of necrosis, and showcases antioxidant capabilities, underlining its cell-regulatory roles. In contrast to doxorubicin’s DNA-centric mechanism, DOX-2 does not interact with nuclear DNA. Given these findings, DOX-2 presents a new promising direction in cancer therapeutics, which is deserving of further in vivo exploration. Full article
(This article belongs to the Special Issue Synthesis and Evaluation of Novel Compounds with Anticancer Activity)
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