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Journal of Enzyme Inhibition and Medicinal Chemistry Volume 35, 2020 - Issue 1
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Research Paper

Cytotoxic substituted indolizines as new colchicine site tubulin polymerisation inhibitors

Monica-Cornelia Sardarua Department of Chemistry, Faculty of Chemistry, “Al. I. Cuza” University of Iasi, Iași, Romania;b “Petru Poni” Institute of Macromolecular Chemistry of Romanian Academy, Iași, RomaniaView further author information
,
Anda Mihaela Craciuna Department of Chemistry, Faculty of Chemistry, “Al. I. Cuza” University of Iasi, Iași, Romania;b “Petru Poni” Institute of Macromolecular Chemistry of Romanian Academy, Iași, RomaniaView further author information
,
Cristina-Maria Al Matarneha Department of Chemistry, Faculty of Chemistry, “Al. I. Cuza” University of Iasi, Iași, Romania;b “Petru Poni” Institute of Macromolecular Chemistry of Romanian Academy, Iași, RomaniaView further author information
,
Isabela Andreea Sandub “Petru Poni” Institute of Macromolecular Chemistry of Romanian Academy, Iași, RomaniaView further author information
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Roxana Maria Amarandia Department of Chemistry, Faculty of Chemistry, “Al. I. Cuza” University of Iasi, Iași, Romania;c TRANSCEND Research Center, Regional Institute of Oncology, Iași, RomaniaORCID Iconhttps://orcid.org/0000-0002-9937-6539View further author information
ORCID Icon,
Lacramioara Popovicia Department of Chemistry, Faculty of Chemistry, “Al. I. Cuza” University of Iasi, Iași, RomaniaView further author information
,
Catalina Ionica Ciobanud Research Department, Faculty of Chemistry, “Al. I. Cuza” University of Iasi, Iași, RomaniaView further author information
,
Dragos Peptanariub “Petru Poni” Institute of Macromolecular Chemistry of Romanian Academy, Iași, RomaniaView further author information
,
Mariana Pintealab “Petru Poni” Institute of Macromolecular Chemistry of Romanian Academy, Iași, RomaniaView further author information
,
Ionel I. Mangalagiua Department of Chemistry, Faculty of Chemistry, “Al. I. Cuza” University of Iasi, Iași, RomaniaORCID Iconhttps://orcid.org/0000-0002-4632-5076View further author information
ORCID Icon &
Ramona Danaca Department of Chemistry, Faculty of Chemistry, “Al. I. Cuza” University of Iasi, Iași, RomaniaCorrespondence[email protected]
ORCID Iconhttps://orcid.org/0000-0003-4370-5353View further author information
ORCID Icon show all
Pages 1581-1595 | Received 17 May 2020, Accepted 19 Jul 2020, Published online: 04 Aug 2020

Figures & data

Figure 1. Design in the series of the target indolizine derivatives.

Figure 1. Design in the series of the target indolizine derivatives.

Figure 2. Effects of compounds 11a, 11b, 11k, 14a, 15a, and 15j (10−5 M) on microtubule dynamics using Paclitaxel (10−5 M) as microtubule stabilising agent and Phenstatin (10−5 M) as microtubule destabilising agent.

Figure 2. Effects of compounds 11a, 11b, 11k, 14a, 15a, and 15j (10−5 M) on microtubule dynamics using Paclitaxel (10−5 M) as microtubule stabilising agent and Phenstatin (10−5 M) as microtubule destabilising agent.

Scheme 1. Synthesis pathway for indolizines 11a–l.

Scheme 1. Synthesis pathway for indolizines 11a–l.

Scheme 2. Synthesis of indolizines 14a–d.

Scheme 2. Synthesis of indolizines 14a–d.

Scheme 3. Synthesis of indolizines 15a–i.

Scheme 3. Synthesis of indolizines 15a–i.

Table 1. Results of the in vitro growth inhibition (GI %) of tested compounds against human cancer cell lines in the single-dose assayTable Footnotea.

Table 2. Results of the 5-dose in vitro human cancer cell growth inhibitionTable Footnotea for compounds 11a, 15a, and 15j and positive control Phenstatin.

Table 3. Binding orientation, energy, and amino acid contacts for tested compounds, as predicted by molecular docking experiments.

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