Synthesis and Antitumor Activity of 1-Substituted 1,2,3-Triazole-Mollugin Derivatives

Luo, Han; Lv, Yue; Zhang, Hong; Hu, Jiang‐Miao; Li, Hongmei; Liu, Shou-Jin

doi:10.3390/molecules26113249

Cited by 8 publications

(2 citation statements)

References 33 publications

(44 reference statements)

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“…Likewise, mollugin, a natural naphthoquinone derivative has been recognized as an interesting anticancer template to halt tumor(s) progression and associated molecular pathogenesis (Wang et al, 2017). As such, Luo et al (2021) established a series of mollugin‐tangled 1,2,3‐triazoles 32 as a target to advance the anticancer leads, as shown in Scheme 8. The copper(I)‐catalyzed click reaction of O ‐propargylated mollugin 30 with classified aryl‐azides 31 furnished mollugin‐1,2,3‐triaoles 32 in efficient yields of 20%–92%.…”

Section: Synthetic Strategiesmentioning

confidence: 99%

Comprehensive review on natural pharmacophore tethered 1,2,3‐triazoles as active pharmaceuticals

Rammohan

Venkatesh²,

Basha

et al. 2022

Chem Biol Drug Des

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The privileged 1,2,3‐triazole scaffold is drawing researcher's attention due to its widespread applications in diverse fields such as drug discovery (e.g., carboxyamidotriazole), organic synthesis (click‐reaction template), polymeric materials (e.g., triazolamer), supramolecular receptors (e.g., triazolophane), fluorescent materials (e.g., metal–organic frameworks), and agricultural sectors (e.g., fungicides). Various 1,2,3‐triazole persuasion modules are also currently available in the market that have multiple assets such as active pharmaceuticals and agricultural purposes. Owed to the highly consistent and firmest synthesis approach, that is, click reaction of various azides and acetylene derivatives by copper (I)‐catalyzed 1,3‐dipolar cycloaddition (CuAAC), highly functionalized 1,2,3‐triazoles are prepared in scalar yields for drug discovery. Given the importance of 1,2,3‐triazole chemistry, the present review focuses specifically on the synthesis of structurally diverse 1,2,3‐triazoles linked to natural pharmacophores and their biological importance. Furthermore, the dual/multi‐pharmacophores assimilated 1,2,3‐triazoles have listed interesting biological activities that could be valuable as future drug leads. In addition, this comprehensive review can serve as a template for the development of new diverse scaffolds that will ensure for new therapeutic approaches for the existing myriad diseases and disorders.

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Section: Synthetic Strategiesmentioning

confidence: 99%

Comprehensive review on natural pharmacophore tethered 1,2,3‐triazoles as active pharmaceuticals

Rammohan

Venkatesh²,

Basha

et al. 2022

Chem Biol Drug Des

View full text Add to dashboard Cite

show abstract

“…1,2,3-Triazole is a nitrogen heterocyclic structural unit that performs an important function in drug design and synthesis . Recently, many studies have shown that compounds with 1,2,3-triazole units show good inhibitory activities against cancer, − inflammation, and microorganisms . Therefore, the synthesis of novel compounds by modifying theophylline with 1,2,3-triazole heterocycles may be an effective strategy for developing potential new chemotherapeutics.…”

Section: Introductionmentioning

confidence: 99%

Carrier-free Nanodrug for the Chemical-Photodynamic Synergistic Treatment of Lung Cancer

Liao,

Ye,

Xie

et al. 2024

ACS Appl. Nano Mater.

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The theophylline derivative d17 is a candidate drug for nonsmall cell lung cancer (NSCLC) treatment previously developed by our group. However, it has the limitations of inadequate bioavailability, poor targeting, and insignificant therapeutic effect. Chemo-photodynamic synergistic therapy is a promising method of synergistic antitumor therapy. Herein, d17 and photosensitizer chlorin e6 (Ce6) were loaded into nanoparticles (NPs) via supramolecular self-assembly, which are selfassembled through π−π stacking and hydrogen bond interactions to form nanospheres with a size of about 85 nm and a surface charge of −33 mV. Compared with free Ce6, the d17−Ce6 NPs have good hydrophilicity and stability and can effectively accumulate in NSCLC tumor tissues due to the enhancement and retention effect. More significantly, the d17−Ce6 NPs can synergistically inhibit tumor growth compared with other treatment groups with no obvious toxicity. Taken together, the d17−Ce6 NPs may be an effective carrier-free nanodrug for the chemophotodynamic synergistic treatment of NSCLC.

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Therapeutic potential of 1,2,3‐triazole hybrids for leukemia treatment

Yang¹,

Xuan²,

Li³

et al. 2022

Archiv der Pharmazie

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Leukemia, a hematological malignancy originating from the bone marrow, is the principal cancer of childhood. In recent decades, improved remission rates and survival of patients with leukemia have been achieved due to significant breakthroughs in the treatment. However, chemoresistance and relapse are common, creating an urgent need for the search for novel pharmaceutical interventions. 1,2,3‐Triazole is one of the most fascinating pharmacophores in the discovery of new drugs, and several 1,2,3‐triazole derivatives have already been used in clinics or are under clinical evaluation for the treatment of cancers. In particular, 1,2,3‐triazole hybrids could suppress tumor proliferation, invasion, and metastasis by inhibiting enzymes, proteins, and receptors in cancer cells, revealing their potential as putative antileukemic agents. This review covers the recent advances regarding the 1,2,3‐triazole hybrids with potential antileukemic activity, focusing on the chemical structures, structure–activity relationship, and mechanisms of action, covering articles published from January 2017 to January 2022.

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Synthesis and Antitumor Activity of 1-Substituted 1,2,3-Triazole-Mollugin Derivatives

Cited by 8 publications

References 33 publications

Comprehensive review on natural pharmacophore tethered 1,2,3‐triazoles as active pharmaceuticals

Comprehensive review on natural pharmacophore tethered 1,2,3‐triazoles as active pharmaceuticals

Carrier-free Nanodrug for the Chemical-Photodynamic Synergistic Treatment of Lung Cancer

Therapeutic potential of 1,2,3‐triazole hybrids for leukemia treatment

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