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Vinca alkaloids used in anticancer therapy are the well-known vinblastine and vincristine as classical antitumor agents. These dimeric molecules consist of two monomers, vindoline and catharanthine, which have no particular activity on their own. The goal in our research work was to obtain derivatives of one of these, vindoline, resulted in molecules with important antiproliferative effect. This type of derivatives were hybrids; vindoline was conjugated with several pharmacophores with and/or without linkers. Pharmacophores were amino acid esters, steroids, triazoles, and flavones. In several cases, the synthesized compounds showed on some cell lines an even better effect than vinblastine.